Chemical modulation of glycerolipid signaling and metabolic pathways

Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids

Volumn 1841, Issue 8, 2014, Pages 1060-1084

  Scott, Sarah A ^a   Mathews, Thomas P ^a   Ivanova, Pavlina T ^a   Lindsley, Craig W ^a,b   Brown, H Alex ^a  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b VANDERBILT UNIVERSITY   (United States)

Author keywords

Autotaxin; Fatty acyltransferase; Glycerolipid; Inhibitor; Lipase; Lipid kinase; Lipin; Metabolism; Phospholipase

Indexed keywords

1 [[6 (3 METHOXYESTRA 1,3,5(10) TRIEN 17BETA YL)AMINO]HEXYL] 1H PYRROLE 2,5 DIONE; 1,6 HEXAMETHYLENEDICARBAMIC ACID BIS(CYCLOHEXANONE OXIME) ESTER; ACYLGLYCEROL LIPASE; ACYLTRANSFERASE; ALPHA BETA HYDROLASE DOMAIN CONTAINING PROTEIN 5; AUTOTAXIN; DIACYLGLYCEROL; DIACYLGLYCEROL ACYLTRANSFERASE 1; DIACYLGLYCEROL ACYLTRANSFERASE 2; DIACYLGLYCEROL KINASE; DIACYLGLYCEROL KINASE INHIBITOR; GLYCEROLIPID; HORMONE SENSITIVE LIPASE; LIPIN; LIPOPROTEIN LIPASE; LYSOPHOSPHATIDIC ACID; LYSOPHOSPHATIDIC ACYLTRANSFERASE; NATURAL PRODUCT; NICOTINIC ACID; PATATIN LIKE PHOSPHOLIPASE DOMAIN CONTAINING PROTEIN; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHOLIPASE A; PHOSPHOLIPASE C; PHOSPHOLIPASE C INHIBITOR; PHOSPHOLIPASE D; PHOSPHOLIPASE D INHIBITOR; PHOSPHOLIPASE INHIBITOR; PROTEIN; SELECTIVE ESTROGEN RECEPTOR MODULATOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

CALCIUM MOBILIZATION; CELL MEMBRANE; DRUG DEVELOPMENT; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; ENERGY METABOLISM; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME MODIFICATION; ENZYME REGULATION; FATTY ACID SYNTHESIS; GLUCOSE METABOLISM; GROWTH RETARDATION; HUMAN; HYPERTRIGLYCERIDEMIA; IC 50; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATION; LIPID METABOLISM; LIPOGENESIS; LIPOTOXICITY; METABOLIC DISORDER; MORTALITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN LIPID INTERACTION; PROTEIN PHOSPHORYLATION; REVIEW; SIGNAL TRANSDUCTION; TISSUE DISTRIBUTION;

AUTOTAXIN; FATTY ACYLTRANSFERASE; GLYCEROLIPID; INHIBITOR; LIPASE; LIPID KINASE; LIPIN; METABOLISM; PHOSPHOLIPASE;

ACYLTRANSFERASES; GLYCEROL; LIPASE; LIPIDS; PHOSPHOLIPASES; PHOSPHORIC MONOESTER HYDROLASES; PHOSPHOTRANSFERASES; SIGNAL TRANSDUCTION;

EID: 84903275752     PISSN: 13881981     EISSN: 18792618     Source Type: Journal    
DOI: 10.1016/j.bbalip.2014.01.009     Document Type: Review

References (359)

1. M.J. Berridge Inositol trisphosphate and diacylglycerol: two interacting second messengers Annu. Rev. Biochem. 56 1987 159 193
2. G. Kadamur, and E.M. Ross Mammalian phospholipase C Annu. Rev. Physiol. 75 2013 127 154
3. M.P. Czech PIP2 and PIP3: complex roles at the cell surface Cell 100 2000 603 606
4. T.K. Harden, G.L. Waldo, S.N. Hicks, and J. Sondek Mechanism of activation and inactivation of Gq/phospholipase C-beta signaling nodes Chem. Rev. 111 2011 6120 6129
5. T.D. Bunney, and M. Katan Phospholipase C epsilon: linking second messengers and small GTPases Trends Cell Biol. 16 2006 640 648 (Pubitemid 44809889)
6. C.M. Vines Phospholipase C Adv. Exp. Med. Biol. 740 2012 235 254
7. G. Berstein, J.L. Blank, D.Y. Jhon, J.H. Exton, S.G. Rhee, and E.M. Ross Phospholipase C-beta 1 is a GTPase-activating protein for Gq/11, its physiologic regulator Cell 70 1992 411 418
8. S. Cockcroft, and G.M. Thomas Inositol-lipid-specific phospholipase C isoenzymes and their differential regulation by receptors Biochem. J. 288 1992 1 14
9. S. Shimohama, Y. Homma, T. Suenaga, S. Fujimoto, T. Taniguchi, W. Araki, Y. Yamaoka, T. Takenawa, and J. Kimura Aberrant accumulation of phospholipase C-delta in Alzheimer brains Am. J. Pathol. 139 1991 737 742
10. K. Fukami, M. Yoshida, T. Inoue, M. Kurokawa, R.A. Fissore, N. Yoshida, K. Mikoshiba, and T. Takenawa Phospholipase Cdelta4 is required for Ca2 + mobilization essential for acrosome reaction in sperm J. Cell Biol. 161 2003 79 88 (Pubitemid 36459081)
11. Y. Nakamura, M. Ichinohe, M. Hirata, H. Matsuura, T. Fujiwara, T. Igarashi, M. Nakahara, H. Yamaguchi, S. Yasugi, T. Takenawa, and K. Fukami Phospholipase C-delta1 is an essential molecule downstream of Foxn1, the gene responsible for the nude mutation, in normal hair development FASEB J. 22 2008 841 849 (Pubitemid 351348136)
12. J.K. Kim, J.W. Choi, S. Lim, O. Kwon, J.K. Seo, S.H. Ryu, and P.G. Suh Phospholipase C-eta1 is activated by intracellular Ca(2 +) mobilization and enhances GPCRs/PLC/Ca(2 +) signaling Cell. Signal. 23 2011 1022 1029
13. G.G. Kelley, S.E. Reks, J.M. Ondrako, and A.V. Smrcka Phospholipase C(epsilon): a novel Ras effector EMBO J. 20 2001 743 754 (Pubitemid 32167639)
14. L. Zhang, S. Malik, J. Pang, H. Wang, K.M. Park, D.I. Yule, B.C. Blaxall, and A.V. Smrcka Phospholipase Cε hydrolyzes perinuclear phosphatidylinositol 4-phosphate to regulate cardiac hypertrophy Cell 153 2013 216 227
15. J.H. Exton Phosphatidylcholine breakdown and signal transduction Biochim. Biophys. Acta 1212 1994 26 42 (Pubitemid 24123885)
16. R.M. Adibhatla, J.F. Hatcher, and A. Gusain Tricyclodecan-9-yl- xanthogenate (D609) mechanism of actions: a mini-review of literature Neurochem. Res. 37 2012 671 679
17. J. Cuschieri, J. Billgren, and R.V. Maier Phosphatidylcholine-specific phospholipase C (PC-PLC) is required for LPS-mediated macrophage activation through CD14 J. Leukoc. Biol. 80 2006 407 414 (Pubitemid 44835514)
18. L. Paris, S. Cecchetti, F. Spadaro, L. Abalsamo, L. Lugini, M.E. Pisanu, E. Iorio, P.G. Natali, C. Ramoni, and F. Podo Inhibition of phosphatidylcholine- specific phospholipase C downregulates HER2 overexpression on plasma membrane of breast cancer cells Breast Cancer Res. 12 2010 R27
19. J.E. Bleasdale, N.R. Thakur, R.S. Gremban, G.L. Bundy, F.A. Fitzpatrick, R.J. Smith, and S. Bunting Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils J. Pharmacol. Exp. Ther. 255 1990 756 768
20. R.J. Smith, L.M. Sam, J.M. Justen, G.L. Bundy, G.A. Bala, and J.E. Bleasdale Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness J. Pharmacol. Exp. Ther. 253 1990 688 697 (Pubitemid 20181715)
21. C. Hou, T. Kirchner, M. Singer, M. Matheis, D. Argentieri, and D. Cavender In vivo activity of a phospholipase C inhibitor, 1-(6-((17beta-3- methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-di one (U73122), in acute and chronic inflammatory reactions J. Pharmacol. Exp. Ther. 309 2004 697 704 (Pubitemid 38542625)
22. R.R. Klein, D.M. Bourdon, C.L. Costales, C.D. Wagner, W.L. White, J.D. Williams, S.N. Hicks, J. Sondek, and D.R. Thakker Direct activation of human phospholipase C by its well known inhibitor u73122 J. Biol. Chem. 286 2011 12407 12416
23. G. Powis, M.J. Seewald, C. Gratas, D. Melder, J. Riebow, and E.J. Modest Selective inhibition of phosphatidylinositol phospholipase C by cytotoxic ether lipid analogues Cancer Res. 52 1992 2835 2840
24. W. Huang, M. Barrett, N. Hajicek, S. Hicks, T.K. Harden, J. Sondek, and Q. Zhang Small molecule inhibitors of phospholipase C from a novel high-throughput screen J. Biol. Chem. 288 2013 5840 5848
25. E. Amtmann, K. Muller-Decker, A. Hoss, G. Schalasta, C. Doppler, and G. Sauer Synergistic antiviral effect of xanthates and ionic detergents Biochem. Pharmacol. 36 1987 1545 1549 (Pubitemid 17079569)
26. E. Amtmann The antiviral, antitumoural xanthate D609 is a competitive inhibitor of phosphatidylcholine-specific phospholipase C Drugs Exp. Clin. Res. 22 1996 287 294 (Pubitemid 27060176)
27. C. Luberto, and Y.A. Hannun Sphingomyelin synthase, a potential regulator of intracellular levels of ceramide and diacylglycerol during SV40 transformation. Does sphingomyelin synthase account for the putative phosphatidylcholine-specific phospholipase C? J. Biol. Chem. 273 1998 14550 14559 (Pubitemid 28319178)
28. D.J. Hanahan, and I.L. Chaikoff A new phospholipide-splitting enzyme specific for the ester linkage between the nitrogenous base and the phosphoric acid grouping J. Biol. Chem. 169 1947 699 705
29. D.J. Hanahan, and I.L. Chaikoff The phosphorus-containing lipides of the carrot J. Biol. Chem. 168 1947 233 240
30. P.E. Selvy, R.R. Lavieri, C.W. Lindsley, and H.A. Brown Phospholipase D: enzymology, functionality, and chemical modulation Chem. Rev. 111 2011 6064 6119
31. M. McDermott, M.J. Wakelam, and A.J. Morris Phospholipase D Biochem. Cell Biol. 82 2004 225 253 (Pubitemid 38580885)
32. C.P. Ponting, and I.D. Kerr A novel family of phospholipase D homologues that includes phospholipid synthases and putative endonucleases: identification of duplicated repeats and potential active site residues Protein Sci. 5 1996 914 922 (Pubitemid 26139179)
33. J.H. Exton Regulation of phospholipase D FEBS Lett. 531 2002 58 61 (Pubitemid 35232785)
34. A.J. Melendez, and J.M. Allen Phospholipase D and immune receptor signalling Semin. Immunol. 14 2002 49 55 (Pubitemid 34250708)
35. S.J. Cook, and M.J. Wakelam Epidermal growth factor increases sn-1,2-diacylglycerol levels and activates phospholipase D-catalysed phosphatidylcholine breakdown in Swiss 3T3 cells in the absence of inositol-lipid hydrolysis Biochem. J. 285 1992 247 253
36. R. Plevin, S.J. Cook, S. Palmer, and M.J. Wakelam Multiple sources of sn-1,2-diacylglycerol in platelet-derived-growth-factor-stimulated Swiss 3T3 fibroblasts. Evidence for activation of phosphoinositidase C and phosphatidylcholine-specific phospholipase D Biochem. J. 279 1991 559 565
37. T.K. Sato, M. Overduin, and S.D. Emr Location, location, location: membrane targeting directed by PX domains Science 294 2001 1881 1885 (Pubitemid 33101577)
38. M.A. Lemmon Pleckstrin homology (PH) domains and phosphoinositides Biochem. Soc. Symp. 2007 81 93
39. L.G. Henage, J.H. Exton, and H.A. Brown Kinetic analysis of a mammalian phospholipase D: allosteric modulation by monomeric GTPases, protein kinase C, and polyphophoinositides J. Biol. Chem. 281 2006 3408 3417 (Pubitemid 43845955)
40. W.E. Hughes, and P.J. Parker Endosomal localization of phospholipase D 1a and 1b is defined by the C-termini of the proteins, and is independent of activity Biochem. J. 356 2001 727 736 (Pubitemid 32588444)
41. G. Du, Y.M. Altshuller, N. Vitale, P. Huang, S. Chasserot-Golaz, A.J. Morris, M.F. Bader, and M.A. Frohman Regulation of phospholipase D1 subcellular cycling through coordination of multiple membrane association motifs J. Cell Biol. 162 2003 305 315 (Pubitemid 36928843)
42. W.C. Colley, T.C. Sung, R. Roll, J. Jenco, S.M. Hammond, Y. Altshuller, D. Bar-Sagi, A.J. Morris, and M.A. Frohman Phospholipase D2, a distinct phospholipase D isoform with novel regulatory properties that provokes cytoskeletal reorganization Curr. Biol. 7 1997 191 201 (Pubitemid 27164725)
43. H.A. Brown, S. Gutowski, C.R. Moomaw, C. Slaughter, and P.C. Sternweis ADP-ribosylation factor, a small GTP-dependent regulatory protein, stimulates phospholipase D activity Cell 75 1993 1137 1144 (Pubitemid 24006110)
44. S. Cockcroft, G.M. Thomas, A. Fensome, B. Geny, E. Cunningham, I. Gout, I. Hiles, N.F. Totty, O. Truong, and J.J. Hsuan Phospholipase D: a downstream effector of ARF in granulocytes Science 263 1994 523 526
45. T.C. Sung, Y.M. Altshuller, A.J. Morris, and M.A. Frohman Molecular analysis of mammalian phospholipase D2 J. Biol. Chem. 274 1999 494 502 (Pubitemid 29035088)
46. W.D. Singer, H.A. Brown, G.M. Bokoch, and P.C. Sternweis Resolved phospholipase D activity is modulated by cytosolic factors other than Arf J. Biol. Chem. 270 1995 14944 14950
47. K.C. Malcolm, A.H. Ross, R.G. Qiu, M. Symons, and J.H. Exton Activation of rat liver phospholipase D by the small GTP-binding protein RhoA J. Biol. Chem. 269 1994 25951 25954 (Pubitemid 24328394)
48. J.H. Exton New developments in phospholipase D J. Biol. Chem. 272 1997 15579 15582 (Pubitemid 27265521)
49. J. Ortmeyer, and V. Mohsenin Inhibition of phospholipase D and superoxide generation by glucose in diabetic neutrophils Life Sci. 59 1996 255 262 (Pubitemid 26201052)
50. H.Y. Lee, K. Yea, J. Kim, B.D. Lee, Y.C. Chae, H.S. Kim, D.W. Lee, S.H. Kim, J.H. Cho, C.J. Jin, D.S. Koh, K.S. Park, P.G. Suh, and S.H. Ryu Epidermal growth factor increases insulin secretion and lowers blood glucose in diabetic mice J. Cell. Mol. Med. 12 2008 1593 1604
51. P.M. Steed, and A.H. Chow Intracellular signaling by phospholipase D as a therapeutic target Curr. Pharm. Biotechnol. 2 2001 241 256 (Pubitemid 32798799)
52. D. Cai, M. Zhong, R. Wang, W.J. Netzer, D. Shields, H. Zheng, S.S. Sisodia, D.A. Foster, F.S. Gorelick, H. Xu, and P. Greengard Phospholipase D1 corrects impaired betaAPP trafficking and neurite outgrowth in familial Alzheimer's disease-linked presenilin-1 mutant neurons Proc. Natl. Acad. Sci. U. S. A. 103 2006 1936 1940 (Pubitemid 43228796)
53. T.G. Oliveira, R.B. Chan, H. Tian, M. Laredo, G. Shui, A. Staniszewski, H. Zhang, L. Wang, T.W. Kim, K.E. Duff, M.R. Wenk, O. Arancio, and G. Di Paolo Phospholipase d2 ablation ameliorates Alzheimer's disease-linked synaptic dysfunction and cognitive deficits J. Neurosci. 30 2010 16419 16428
54. N. Uchida, S. Okamura, and H. Kuwano Phospholipase D activity in human gastric carcinoma Anticancer Res 19 1999 671 675 (Pubitemid 29168314)
55. D.Y. Noh, S.J. Ahn, R.A. Lee, I.A. Park, J.H. Kim, P.G. Suh, S.H. Ryu, K.H. Lee, and J.S. Han Overexpression of phospholipase D1 in human breast cancer tissues Cancer Lett. 161 2000 207 214
56. N. Uchida, S. Okamura, Y. Nagamachi, and S. Yamashita Increased phospholipase D activity in human breast cancer J. Cancer Res. Clin. Oncol. 123 1997 280 285 (Pubitemid 27230904)
57. Y. Yamada, N. Hamajima, T. Kato, H. Iwata, Y. Yamamura, M. Shinoda, M. Suyama, T. Mitsudomi, K. Tajima, S. Kusakabe, H. Yoshida, Y. Banno, Y. Akao, M. Tanaka, and Y. Nozawa Association of a polymorphism of the phospholipase D2 gene with the prevalence of colorectal cancer J. Mol. Med. 81 2003 126 131 (Pubitemid 36313238)
58. M.H. Park, B.H. Ahn, Y.K. Hong, and S. Min do Overexpression of phospholipase D enhances matrix metalloproteinase-2 expression and glioma cell invasion via protein kinase C and protein kinase A/NF-kappaB/Sp1-mediated signaling pathways Carcinogenesis 30 2009 356 365
59. Y. Zhao, H. Ehara, Y. Akao, M. Shamoto, Y. Nakagawa, Y. Banno, T. Deguchi, N. Ohishi, K. Yagi, and Y. Nozawa Increased activity and intranuclear expression of phospholipase D2 in human renal cancer Biochem. Biophys. Res. Commun. 278 2000 140 143
60. W. Su, Q. Chen, and M.A. Frohman Targeting phospholipase D with small-molecule inhibitors as a potential therapeutic approach for cancer metastasis Future Oncol. 5 2009 1477 1486
61. P. Huang, and M.A. Frohman The potential for phospholipase D as a new therapeutic target Expert Opin. Ther. Targets 11 2007 707 716 (Pubitemid 46730084)
62. C.W. Lindsley, and H.A. Brown Phospholipase D as a therapeutic target in brain disorders Neuropsychopharmacology 37 2012 301 302
63. R.M. Dawson The formation of phosphatidylglycerol and other phospholipids by the transferase activity of phospholipase D Biochem. J. 102 1967 205 210
64. S.F. Yang, S. Freer, and A.A. Benson Transphosphatidylation by phospholipase D J. Biol. Chem. 242 1967 477 484
65. R.W. Randall, R.W. Bonser, N.T. Thompson, and L.G. Garland A novel and sensitive assay for phospholipase D in intact cells FEBS Lett. 264 1990 87 90 (Pubitemid 20139813)
66. L. Seidler, M. Kaszkin, and V. Kinzel Primary alcohols and phosphatidylcholine metabolism in rat brain synaptosomal membranes via phospholipase D Pharmacol. Toxicol. 78 1996 249 253 (Pubitemid 26107867)
67. E. Kobayashi, H. Nakano, M. Morimoto, and T. Tamaoki Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C Biochem. Biophys. Res. Commun. 159 1989 548 553 (Pubitemid 19089785)
68. X.L. Zheng, Y. Gui, G. Du, M.A. Frohman, and D.Q. Peng Calphostin-C induction of vascular smooth muscle cell apoptosis proceeds through phospholipase D and microtubule inhibition J. Biol. Chem. 279 2004 7112 7118 (Pubitemid 38248858)
69. J. Tou, and C. Urbizo Resveratrol inhibits the formation of phosphatidic acid and diglyceride in chemotactic peptide- or phorbol ester-stimulated human neutrophils Cell. Signal. 13 2001 191 197 (Pubitemid 32244403)
70. J.S. Tou, and C. Urbizo Diethylstilbestrol inhibits phospholipase D activity and degranulation by stimulated human neutrophils Steroids 73 2008 216 221
71. A. Garcia, Y. Zheng, C. Zhao, A. Toschi, J. Fan, N. Shraibman, H.A. Brown, D. Bar-Sagi, D.A. Foster, and J.L. Arbiser Honokiol suppresses survival signals mediated by Ras-dependent phospholipase D activity in human cancer cells Clin. Cancer Res. 14 2008 4267 4274
72. M.S. Puar, E. Barrabee, M. Hallade, and M. Patel Sch 420789: a novel fungal metabolite with phospholipase D inhibitory activity J. Antibiot. 53 2000 837 838
73. J.K. Pai, E.A. Frank, C. Blood, and M. Chu Novel ketoepoxides block phospholipase D activation and tumor cell invasion Anticancer Drug Des. 9 1994 363 372 (Pubitemid 24297532)
74. L.A. McDonald, L.R. Barbieri, V.S. Bernan, J. Janso, P. Lassota, and G.T. Carter 07H239-A, a new cytotoxic eremophilane sesquiterpene from the marine-derived Xylariaceous fungus LL-07H239 J. Nat. Prod. 67 2004 1565 1567 (Pubitemid 39298628)
75. B.D. Levy, L. Hickey, A.J. Morris, M. Larvie, R. Keledjian, N.A. Petasis, G. Bannenberg, and C.N. Serhan Novel polyisoprenyl phosphates block phospholipase D and human neutrophil activation in vitro and murine peritoneal inflammation in vivo Br. J. Pharmacol. 146 2005 344 351 (Pubitemid 41486676)
76. B.D. Levy, V.V. Fokin, J.M. Clark, M.J. Wakelam, N.A. Petasis, and C.N. Serhan Polyisoprenyl phosphate (PIPP) signaling regulates phospholipase D activity: a 'stop' signaling switch for aspirin-triggered lipoxin A4 FASEB J. 13 1999 903 911 (Pubitemid 29220702)
77. S.F. Eisen, and H.A. Brown Selective estrogen receptor (ER) modulators differentially regulate phospholipase D catalytic activity in ER-negative breast cancer cells Mol. Pharmacol. 62 2002 911 920
78. L. Monovich, B. Mugrage, E. Quadros, K. Toscano, R. Tommasi, S. LaVoie, E. Liu, Z. Du, D. LaSala, W. Boyar, and P. Steed Optimization of halopemide for phospholipase D2 inhibition Bioorg. Med. Chem. Lett. 17 2007 2310 2311 (Pubitemid 46484301)
79. A.J. Loonen, I. van Wijngaarden, P.A. Janssen, and W. Soudijn Regional localization of halopemide, a new psychotropic agent, in the rat brain Eur. J. Pharmacol. 50 1978 403 408 (Pubitemid 9220140)
80. W. Su, O. Yeku, S. Olepu, A. Genna, J.S. Park, H. Ren, G. Du, M.H. Gelb, A.J. Morris, and M.A. Frohman 5-Fluoro-2-indolyl des-chlorohalopemide (FIPI), a phospholipase D pharmacological inhibitor that alters cell spreading and inhibits chemotaxis Mol. Pharmacol. 75 2009 437 446
81. D. Faugaret, F.C. Chouinard, D. Harbour, M.A. El azreq, and S.G. Bourgoin An essential role for phospholipase D in the recruitment of vesicle amine transport protein-1 to membranes in human neutrophils Biochem. Pharmacol. 81 2011 144 156
82. M. Elvers, M. Grenegård, H. Khoshjabinzadeh, P. Münzer, O. Borst, H. Tian, G. Di Paolo, F. Lang, M. Gawaz, T.L. Lindahl, and K. Fälker A novel role for phospholipase D as an endogenous negative regulator of platelet sensitivity Cell. Signal. 24 2012 1743 1752
83. D. Stegner, I. Thielmann, P. Kraft, M.A. Frohman, G. Stoll, and B. Nieswandt Pharmacological inhibition of phospholipase D protects mice from occlusive thrombus formation and ischemic stroke - brief report Arterioscler. Thromb. Vasc. Biol. 33 2013 2212 2217
84. S.A. Scott, P.E. Selvy, J.R. Buck, H.P. Cho, T.L. Criswell, A.L. Thomas, M.D. Armstrong, C.L. Arteaga, C.W. Lindsley, and H.A. Brown Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness Nat. Chem. Biol. 5 2009 108 117
85. J.A. Lewis, S.A. Scott, R. Lavieri, J.R. Buck, P.E. Selvy, S.L. Stoops, M.D. Armstrong, H.A. Brown, and C.W. Lindsley Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity Bioorg. Med. Chem. Lett. 19 2009 1916 1920
86. R.R. Lavieri, S.A. Scott, P.E. Selvy, K. Kim, S. Jadhav, R.D. Morrison, J.S. Daniels, H.A. Brown, and C.W. Lindsley Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl) ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor J. Med. Chem. 53 2010 6706 6719
87. R.R. Lavieri, S.A. Scott, J.A. Lewis, P.E. Selvy, M.D. Armstrong, H.A. Brown, and C.W. Lindsley Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan- 4-one privileged structure that engenders PLD2 selectivity Bioorg. Med. Chem. Lett. 19 2009 2240 2243
88. M.C. O'Reilly, S.A. Scott, K.A. Brown, T.H. Oguin 3rd, P.G. Thomas, J.S. Daniels, R. Morrison, H.A. Brown, and C.W. Lindsley Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells J. Med. Chem. 56 2013 2695 2699
89. J. Aoki, A. Inoue, K. Makide, N. Saiki, and H. Arai Structure and function of extracellular phospholipase A1 belonging to the pancreatic lipase gene family Biochimie 89 2007 197 204 (Pubitemid 46161954)
90. J. Aoki, Y. Nagai, H. Hosono, K. Inoue, and H. Arai Structure and function of phosphatidylserine-specific phospholipase A1 Biochim. Biophys. Acta 1582 2002 26 32
91. M. Murakami, Y. Taketomi, Y. Miki, H. Sato, T. Hirabayashi, and K. Yamamoto Recent progress in phospholipase A(2) research: from cells to animals to humans Prog. Lipid Res. 50 2011 152 192
92. J.E. Burke, and E.A. Dennis Phospholipase A2 structure/function, mechanism, and signaling J. Lipid Res. 50 2009 S237 S242
93. J.E. Burke, and E.A. Dennis Phospholipase A2 biochemistry Cardiovasc. Drugs Ther. 23 2009 49 59
94. G. Lambeau, and M.H. Gelb Biochemistry and physiology of mammalian secreted phospholipases A2 Annu. Rev. Biochem. 77 2008 495 520
95. E.A. Dennis, J. Cao, Y.H. Hsu, V. Magrioti, and G. Kokotos Phospholipase A2 enzymes: physical structure, biological function, disease implication, chemical inhibition, and therapeutic intervention Chem. Rev. 111 2011 6130 6185
96. S.A. Karabina, S. Gora, R. Atout, and E. Ninio Extracellular phospholipases in atherosclerosis Biochimie 92 2010 594 600
97. M. Ghosh, D.E. Tucker, S.A. Burchett, and C.C. Leslie Properties of the Group IV phospholipase A2 family Prog. Lipid Res. 45 2006 487 510
98. R.J. Flower The development of COX2 inhibitors Nat. Rev. Drug Discov. 2 2003 179 191 (Pubitemid 37361663)
99. J.F. Carlquist, J.B. Muhlestein, and J.L. Anderson Lipoprotein-associated phospholipase A2: a new biomarker for cardiovascular risk assessment and potential therapeutic target Expert Rev. Mol. Diagn. 7 2007 511 517 (Pubitemid 47547719)
100. V. Magrioti, and G. Kokotos Phospholipase A2 inhibitors as potential therapeutic agents for the treatment of inflammatory diseases Expert Opin. Ther. Pat. 20 2010 1 18
101. D.W. Snyder, N.J. Bach, R.D. Dillard, S.E. Draheim, D.G. Carlson, N. Fox, N.W. Roehm, C.T. Armstrong, C.H. Chang, L.W. Hartley, L.M. Johnson, C.R. Roman, A.C. Smith, M. Song, and J.H. Fleisch Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: a new class of anti-inflammatory drugs, SPI J. Pharmacol. Exp. Ther. 288 1999 1117 1124 (Pubitemid 29254149)
102. M. Karakas, and W. Koenig Varespladib methyl, an oral phospholipase A2 inhibitor for the potential treatment of coronary artery disease IDrugs 12 2009 585 592
103. K.L. Lee, M.A. Foley, L. Chen, M.L. Behnke, F.E. Lovering, S.J. Kirincich, W. Wang, J. Shim, S. Tam, M.W. Shen, S. Khor, X. Xu, D.G. Goodwin, M.K. Ramarao, C. Nickerson-Nutter, F. Donahue, M.S. Ku, J.D. Clark, and J.C. McKew Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha J. Med. Chem. 50 2007 1380 1400 (Pubitemid 46504977)
104. J.C. McKew, K.L. Lee, M.W. Shen, P. Thakker, M.A. Foley, M.L. Behnke, B. Hu, F.W. Sum, S. Tam, Y. Hu, L. Chen, S.J. Kirincich, R. Michalak, J. Thomason, M. Ipek, K. Wu, L. Wooder, M.K. Ramarao, E.A. Murphy, D.G. Goodwin, L. Albert, X. Xu, F. Donahue, M.S. Ku, J. Keith, C.L. Nickerson-Nutter, W.M. Abraham, C. Williams, M. Hegen, and J.D. Clark Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl) -1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib J. Med. Chem. 51 2008 3388 3413 (Pubitemid 351874997)
105. J.C. McKew, K.L. Lee, L. Chen, R. Vargas, J.D. Clark, C. Williams, V. Clerin, S. Marusic, and K. Pong Inhibitors of cytosolic phospholipase A2 U.S. Patent, vol. US7557135B2 2006 USA
106. D. Thotala, J.M. Craft, D.J. Ferraro, R.P. Kotipatruni, S.R. Bhave, J.J. Jaboin, and D.E. Hallahan Cytosolic phospholipaseA2 inhibition with PLA-695 radiosensitizes tumors in lung cancer animal models PLoS One 8 2013 e69688
107. C. Baskakis, V. Magrioti, N. Cotton, D. Stephens, V. Constantinou- Kokotou, E.A. Dennis, and G. Kokotos Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes J. Med. Chem. 51 2008 8027 8037
108. G. Kokotos, Y.H. Hsu, J.E. Burke, C. Baskakis, C.G. Kokotos, V. Magrioti, and E.A. Dennis Potent and selective fluoroketone inhibitors of group VIA calcium-independent phospholipase A2 J. Med. Chem. 53 2010 3602 3610
109. V. Magrioti, A. Nikolaou, A. Smyrniotou, I. Shah, V. Constantinou- Kokotou, E.A. Dennis, and G. Kokotos New potent and selective polyfluoroalkyl ketone inhibitors of GVIA calcium-independent phospholipase A Bioorg. Med. Chem. 21 2013 5823 5829
110. J.A. Blackie, J.C. Bloomer, M.J. Brown, H.Y. Cheng, B. Hammond, D.M. Hickey, R.J. Ife, C.A. Leach, V.A. Lewis, C.H. Macphee, K.J. Milliner, K.E. Moores, I.L. Pinto, S.A. Smith, I.G. Stansfield, S.J. Stanway, M.A. Taylor, and C.J. Theobald The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2 Bioorg. Med. Chem. Lett. 13 2003 1067 1070 (Pubitemid 36331801)
111. H.M. Garcia-Garcia, R.M. Oemrawsingh, S. Brugaletta, P. Vranckx, J. Shannon, R. Davies, E. Boersma, and P.W. Serruys Darapladib effect on circulating high sensitive troponin in patients with acute coronary syndromes Atherosclerosis 225 2012 142 147
112. J.A. Boutin, and G. Ferry Autotaxin Cell. Mol. Life Sci. 66 2009 3009 3021
113. S. Jansen, C. Stefan, J.W. Creemers, E. Waelkens, A. Van Eynde, W. Stalmans, and M. Bollen Proteolytic maturation and activation of autotaxin (NPP2), a secreted metastasis-enhancing lysophospholipase D J. Cell Sci. 118 2005 3081 3089 (Pubitemid 41149912)
114. J. Hausmann, S. Kamtekar, E. Christodoulou, J.E. Day, T. Wu, Z. Fulkerson, H.M. Albers, L.A. van Meeteren, A.J. Houben, L. van Zeijl, S. Jansen, M. Andries, T. Hall, L.E. Pegg, T.E. Benson, M. Kasiem, K. Harlos, C.W. Kooi, S.S. Smyth, H. Ovaa, M. Bollen, A.J. Morris, W.H. Moolenaar, and A. Perrakis Structural basis of substrate discrimination and integrin binding by autotaxin Nat. Struct. Mol. Biol. 18 2011 198 204
115. H. Nishimasu, S. Okudaira, K. Hama, E. Mihara, N. Dohmae, A. Inoue, R. Ishitani, J. Takagi, J. Aoki, and O. Nureki Crystal structure of autotaxin and insight into GPCR activation by lipid mediators Nat. Struct. Mol. Biol. 18 2011 205 212
116. H.M. Albers, and H. Ovaa Chemical evolution of autotaxin inhibitors Chem. Rev. 112 2012 2593 2603
117. J.W. Choi, D.R. Herr, K. Noguchi, Y.C. Yung, C.W. Lee, T. Mutoh, M.E. Lin, S.T. Teo, K.E. Park, A.N. Mosley, and J. Chun LPA receptors: subtypes and biological actions Annu. Rev. Pharmacol. Toxicol. 50 2010 157 186
118. A.J. Houben, and W.H. Moolenaar Autotaxin and LPA receptor signaling in cancer Cancer Metastasis Rev. 30 2011 557 565
119. C. Stortelers, R. Kerkhoven, and W.H. Moolenaar Multiple actions of lysophosphatidic acid on fibroblasts revealed by transcriptional profiling BMC Genomics 9 2008 387
120. L. Federico, Z. Pamuklar, S.S. Smyth, and A.J. Morris Therapeutic potential of autotaxin/lysophospholipase d inhibitors Curr. Drug Targets 9 2008 698 708
121. S. Liu, M. Umezu-Goto, M. Murph, Y. Lu, W. Liu, F. Zhang, S. Yu, L.C. Stephens, X. Cui, G. Murrow, K. Coombes, W. Muller, M.C. Hung, C.M. Perou, A.V. Lee, X. Fang, and G.B. Mills Expression of autotaxin and lysophosphatidic acid receptors increases mammary tumorigenesis, invasion, and metastases Cancer Cell 15 2009 539 550
122. S. Willier, E. Butt, and T.G. Grunewald Lysophosphatidic acid (LPA) signalling in cell migration and cancer invasion: a focussed review and analysis of LPA receptor gene expression on the basis of more than 1700 cancer microarrays Biol. Cell 2013 317 333
123. E. Barbayianni, V. Magrioti, P. Moutevelis-Minakakis, and G. Kokotos Autotaxin inhibitors: a patent review Expert Opin. Ther. Pat. 23 2013 1123 1132
124. L.A. van Meeteren, V. Brinkmann, J.S. Saulnier-Blache, K.R. Lynch, and W.H. Moolenaar Anticancer activity of FTY720: phosphorylated FTY720 inhibits autotaxin, a metastasis-enhancing and angiogenic lysophospholipase D Cancer Lett. 266 2008 203 208
125. G. Ferry, N. Moulharat, J.P. Pradere, P. Desos, A. Try, A. Genton, A. Giganti, M. Beucher-Gaudin, M. Lonchampt, M. Bertrand, J.S. Saulnier-Blache, G.C. Tucker, A. Cordi, and J.A. Boutin S32826, a nanomolar inhibitor of autotaxin: discovery, synthesis and applications as a pharmacological tool J. Pharmacol. Exp. Ther. 327 2008 809 819
126. D.L. Baker, Y. Fujiwara, K.R. Pigg, R. Tsukahara, S. Kobayashi, H. Murofushi, A. Uchiyama, K. Murakami-Murofushi, E. Koh, R.W. Bandle, H.S. Byun, R. Bittman, D. Fan, M. Murph, G.B. Mills, and G. Tigyi Carba analogs of cyclic phosphatidic acid are selective inhibitors of autotaxin and cancer cell invasion and metastasis J. Biol. Chem. 281 2006 22786 22793
127. G. Jiang, Y. Xu, Y. Fujiwara, T. Tsukahara, R. Tsukahara, J. Gajewiak, G. Tigyi, and G.D. Prestwich Alpha-substituted phosphonate analogues of lysophosphatidic acid (LPA) selectively inhibit production and action of LPA ChemMedChem 2 2007 679 690
128. J. Gierse, A. Thorarensen, K. Beltey, E. Bradshaw-Pierce, L. Cortes-Burgos, T. Hall, A. Johnston, M. Murphy, O. Nemirovskiy, S. Ogawa, L. Pegg, M. Pelc, M. Prinsen, M. Schnute, J. Wendling, S. Wene, R. Weinberg, A. Wittwer, B. Zweifel, and J. Masferrer A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation J. Pharmacol. Exp. Ther. 334 2010 310 317
129. H.M. Albers, L.A. van Meeteren, D.A. Egan, E.W. van Tilburg, W.H. Moolenaar, and H. Ovaa Discovery and optimization of boronic acid based inhibitors of autotaxin J. Med. Chem. 53 2010 4958 4967
130. H.M. Albers, A. Dong, L.A. van Meeteren, D.A. Egan, M. Sunkara, E.W. van Tilburg, K. Schuurman, O. van Tellingen, A.J. Morris, S.S. Smyth, W.H. Moolenaar, and H. Ovaa Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation Proc. Natl. Acad. Sci. U. S. A. 107 2010 7257 7262
131. J.I. Fells, S.C. Lee, Y. Fujiwara, D.D. Norman, K.G. Lim, R. Tsukahara, J. Liu, R. Patil, D.D. Miller, R.J. Kirby, S. Nelson, W. Seibel, R. Papoian, A.L. Parrill, D.L. Baker, R. Bittman, and G. Tigyi Hits of a high-throughput screen identify the hydrophobic pocket of autotaxin/lysophospholipase D as an inhibitory surface Mol. Pharmacol. 84 2013 415 424
132. M.K. Topham, and R.M. Epand Mammalian diacylglycerol kinases: molecular interactions and biological functions of selected isoforms Biochim. Biophys. Acta 90 2009 416 424
133. Y.V. Shulga, M.K. Topham, and R.M. Epand Regulation and functions of diacylglycerol kinases Chem. Rev. 111 2011 6186 6208
134. A. Ávila-Flores, T. Santos, E. Rincón, and I. Mérida Modulation of the mammalian target of rapamycin pathway by diacylglycerol kinase-produced phosphatidic acid J. Biol. Chem. 280 2005 10091 10099 (Pubitemid 40395861)
135. C. Delon, M. Manifava, E. Wood, D. Thompson, S. Krugmann, S. Pyne, and N.T. Ktistakis Sphingosine kinase 1 is an intracellular effector of phosphatidic acid J. Biol. Chem. 279 2004 44763 44774 (Pubitemid 39430887)
136. B. Luo, S.M. Prescott, and M.K. Topham Diacylglycerol kinase zeta regulates phosphatidylinositol 4-phosphate 5-kinase Ialpha by a novel mechanism Cell. Signal. 16 2004 891 897 (Pubitemid 38638779)
137. A.C. Newton Protein kinase C: poised to signal Am. J. Physiol. Endocrinol. Metab. 298 2010 E395 E402
138. K. Yamada, F. Sakane, N. Matsushima, and H. Kanoh EF-hand motifs of alpha, beta and gamma isoforms of diacylglycerol kinase bind calcium with different affinities and conformational changes Biochem. J. 321 1997 59 64 (Pubitemid 27032569)
139. F. Sakane, K. Yamada, and H. Kanoh Different effects of sphingosine, R59022 and anionic amphiphiles on two diacylglycerol kinase isozymes purified from porcine thymus cytosol FEBS Lett. 255 1989 409 413 (Pubitemid 19234535)
140. H. Takeuchi, T. Kanematsu, Y. Misumi, F. Sakane, H. Konishi, U. Kikkawa, Y. Watanabe, M. Katan, and M. Hirata Distinct specificity in the binding of inositol phosphates by pleckstrin homology domains of pleckstrin, RAC-protein kinase, diacylglycerol kinase and a new 130 kDa protein Biochim. Biophys. Acta 1359 1997 275 285 (Pubitemid 28027125)
141. S. Thirugnanam, M.K. Topham, and R.M. Epand Physiological implications of the contrasting modulation of the activities of the epsilon- and zeta-isoforms of diacylglycerol kinase Biochemistry 40 2001 10607 10613 (Pubitemid 32816672)
142. B. Luo, S.M. Prescott, and M.K. Topham Association of diacylglycerol kinase zeta with protein kinase C alpha: spatial regulation of diacylglycerol signaling J. Cell Biol. 160 2003 929 937 (Pubitemid 36350847)
143. B. Houssa, J. de Widt, O. Kranenburg, W.H. Moolenaar, and W.J. van Blitterswijk Diacylglycerol kinase theta binds to and is negatively regulated by active RhoA J. Biol. Chem. 274 1999 6820 6822
144. N. Kobayashi, Y. Hozumi, T. Ito, T. Hosoya, H. Kondo, and K. Goto Differential subcellular targeting and activity-dependent subcellular localization of diacylglycerol kinase isozymes in transfected cells Eur. J. Cell Biol. 86 2007 433 444 (Pubitemid 47099508)
145. T. Murakami, F. Sakane, S. Imai, K. Houkin, and H. Kanoh Identification and characterization of two splice variants of human diacylglycerol kinase eta J. Biol. Chem. 278 2003 34364 34372 (Pubitemid 37553281)
146. S.B. Milne, P.T. Ivanova, M.D. Armstrong, D.S. Myers, J. Lubarda, Y.V. Shulga, M.K. Topham, H.A. Brown, and R.M. Epand Dramatic differences in the roles in lipid metabolism of two isoforms of diacylglycerol kinase Biochemistry 47 2008 9372 9379
147. M. Lung, Y.V. Shulga, P.T. Ivanova, D.S. Myers, S.B. Milne, H.A. Brown, M.K. Topham, and R.M. Epand Diacylglycerol kinase epsilon is selective for both acyl chains of phosphatidic acid or diacylglycerol J. Biol. Chem. 284 2009 31062 31073
148. Y.V. Shulga, D. Loukov, P.T. Ivanova, S.B. Milne, D.S. Myers, G.M. Hatch, G. Umeh, D. Jalan, M.D. Fullerton, G.R. Steinberg, M.K. Topham, H.A. Brown, and R.M. Epand Diacylglycerol kinase delta promotes lipogenesis Biochemistry 52 2013 7766 7776
149. W.R. Bishop, B.R. Ganong, and R.M. Bell Attenuation of sn-1,2-diacylglycerol second messengers by diacylglycerol kinase. Inhibition by diacylglycerol analogs in vitro and in human platelets J. Biol. Chem. 261 1986 6993 7000 (Pubitemid 17219472)
150. D.C. de Chaffoy de Courcelles, P. Roevens, and H. Van Belle R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet J. Biol. Chem. 260 1985 15762 15770 (Pubitemid 16173206)
151. D. de Chaffoy de Courcelles, P. Roevens, H. Van Belle, L. Kennis, Y. Somers, and F. De Clerck The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949 J. Biol. Chem. 264 1989 3274 3285 (Pubitemid 19063384)
152. B. Rodriguez-Linares, T. Walker, and S. Watson The diacylglycerol kinase inhibitor, R59949, potentiates secretion but not increased phosphorylation of a 47 kDalton protein in human platelets Biochem. Pharmacol. 41 1991 835 838
153. Y. Jiang, F. Sakane, H. Kanoh, and J.P. Walsh Selectivity of the diacylglycerol kinase inhibitor 3-[2-(4-[bis-(4-fluorophenyl)methylene]-1- piperidinyl)ethyl]-2, 3-dihydro-2-thioxo-4(1H)quinazolinone (R59949) among diacylglycerol kinase subtypes Biochem. Pharmacol. 59 2000 763 772 (Pubitemid 30081699)
154. Y. Zha, R. Marks, A.W. Ho, A.C. Peterson, S. Janardhan, I. Brown, K. Praveen, S. Stang, J.C. Stone, and T.F. Gajewski T cell anergy is reversed by active Ras and is regulated by diacylglycerol kinase-alpha Nat. Immunol. 7 2006 1166 1173 (Pubitemid 44594312)
155. S.A. Scott, Y. Xiang, T.P. Mathews, H.C. Plumley, D.S. Myers, M.D. Armstrong, K.A. Tallman, M.C. O'Reilly, C.W. Lindsley, and H.A. Brown Regulation of Phospholipase D activity and phosphatidic acid production following purinergic (P2Y6) receptor stimulation J. Biol. Chem. 288 2013 20477 20487
156. N. Sadeghi, and D.E. Gerber Targeting the PI3K pathway for cancer therapy Future Med. Chem. 4 2012 1153 1169
157. B. Karakas, K.E. Bachman, and B.H. Park Mutation of the PIK3CA oncogene in human cancers Brit. J. Cancer 94 2006 455 459 (Pubitemid 43289745)
158. M.P. Wymann, and C. Schultz The chemical biology of phosphoinositide 3-kinases Chembiochem 13 2012 2022 2035
159. J.A. Engelman, J. Luo, and L.C. Cantley The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism Nat. Rev. Genet. 7 2006 606 619 (Pubitemid 44100518)
160. J. Rodon, R. Dienstmann, V. Serra, and J. Tabernero Development of PI3K inhibitors: lessons learned from early clinical trials Nat. Rev. Clin. Oncol. 10 2013 143 153
161. S.M. Schultze, B.A. Hemmings, M. Niessen, and O. Tschopp PI3K/AKT, MAPK and AMPK signalling: protein kinases in glucose homeostasis Expert Rev. Mol. Med. 14 2012 e1
162. J.E. Kurtz, and I. Ray-Coquard PI3 kinase inhibitors in the clinic: an update Anticancer Res 32 2012 2463 2470
163. C.J. Vlahos, W.F. Matter, K.Y. Hui, and R.F. Brown A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4- one (LY294002) J. Biol. Chem. 269 1994 5241 5248
164. G. Powis, R. Bonjouklian, M.M. Berggren, A. Gallegos, R. Abraham, C. Ashendel, L. Zalkow, W.F. Matter, J. Dodge, G. Grindey, and C.J. Vlahos Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase Cancer Res. 54 1994 2419 2423
165. M.P. Wymann, G. Bulgarelli-Leva, M.J. Zvelebil, L. Pirola, B. Vanhaesebroeck, M.D. Waterfield, and G. Panayotou Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction Mol. Cell. Biol. 16 1996 1722 1733 (Pubitemid 26095645)
166. E.H. Walker, M.E. Pacold, O. Perisic, L. Stephens, P.T. Hawkins, M.P. Wymann, and R.L. Williams Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine Mol. Cell 6 2000 909 919
167. M. Karlsson, J.A. Contreras, U. Hellman, H. Tornqvist, and C. Holm cDNA cloning, tissue distribution, and identification of the catalytic triad of monoglyceride lipase. Evolutionary relationship to esterases, lysophospholipases, and haloperoxidases J. Biol. Chem. 272 1997 27218 27223 (Pubitemid 27452682)
168. J.Z. Long, D.K. Nomura, and B.F. Cravatt Characterization of monoacylglycerol lipase inhibition reveals differences in central and peripheral endocannabinoid metabolism Chem. Biol. 16 2009 744 753
169. T. Bertrand, F. Augé, J. Houtmann, A. Rak, F. Vallée, V. Mikol, P. Berne, N. Michot, D. Cheuret, C. Hoornaert, and M. Mathieu Structural basis for human monoglyceride lipase inhibition J. Mol. Biol. 396 2010 663 673
170. S. Munro, K.L. Thomas, and M. Abu-Shaar Molecular characterization of a peripheral receptor for cannabinoids Nature 365 1993 61 65 (Pubitemid 23305569)
171. T.P. Dinh, D. Carpenter, F.M. Leslie, T.F. Freund, I. Katona, S.L. Sensi, S. Kathuria, and D. Piomelli Brain monoglyceride lipase participating in endocannabinoid inactivation Proc. Natl. Acad. Sci. U. S. A. 99 2002 10819 10824
172. J.Z. Long, W. Li, L. Booker, J.J. Burston, S.G. Kinsey, J.E. Schlosburg, F.J. Pavón, A.M. Serrano, D.E. Selley, L.H. Parsons, A.H. Lichtman, and B.F. Cravatt Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects Nat. Chem. Biol. 5 2008 37 44
173. M.W. Buczynski, D.S. Dumlao, and E.A. Dennis Thematic Review Series: Proteomics. An integrated omics analysis of eicosanoid biology J. Lipid Res. 50 2009 1015 1038
174. T.A. Rosenberger, N.E. Villacreses, M.A. Contreras, J.V. Bonventre, and S.I. Rapoport Brain lipid metabolism in the cPLA2 knockout mouse J. Lipid Res. 44 2003 109 117 (Pubitemid 36114776)
175. D.K. Nomura, B.E. Morrison, J.L. Blankman, J.Z. Long, S.G. Kinsey, M.C. Marcondes, A.M. Ward, Y.K. Hahn, A.H. Lichtman, B. Conti, and B.F. Cravatt Endocannabinoid hydrolysis generates brain prostaglandins that promote neuroinflammation Science 334 2011 809 813
176. D.K. Nomura, J.Z. Long, S. Niessen, H.S. Hoover, S. Ng, and B.F. Cravatt Monoacylglycerol lipase regulates a fatty acid network that promotes cancer pathogenesis Cell 140 2010 49 61
177. D. Nomura, D. Lombardi, J. Chang, S. Niessen, A. Ward, J. Long, H. Hoover, and B. Cravatt Monoacylglycerol lipase exerts dual control over endocannabinoid and fatty acid pathways to support prostate cancer Chem. Biol. 18 2011 846 856
178. A.G. Hohmann, R.L. Suplita, N.M. Bolton, M.H. Neely, D. Fegley, R. Mangieri, J.F. Krey, J.M. Walker, P.V. Holmes, J.D. Crystal, A. Duranti, A. Tontini, M. Mor, G. Tarzia, and D. Piomelli An endocannabinoid mechanism for stress-induced analgesia Nature 435 2005 1108 1112 (Pubitemid 40910518)
179. B.F. Cravatt, D.K. Giang, S.P. Mayfield, D.L. Boger, R.A. Lerner, and N.B. Gilula Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides Nature 384 1996 83 87 (Pubitemid 26374593)
180. S. Vandevoorde, K.O. Jonsson, G. Labar, E. Persson, D.M. Lambert, and C.J. Fowler Lack of selectivity of URB602 for 2-oleoylglycerol compared to anandamide hydrolysis in vitro Br. J. Pharmacol. 150 2007 186 191 (Pubitemid 46160608)
181. A.R. King, A. Duranti, A. Tontini, S. Rivara, A. Rosengarth, J.R. Clapper, G. Astarita, J.A. Geaga, H. Luecke, M. Mor, G. Tarzia, and D. Piomelli URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices Chem. Biol. 14 2007 1357 1365 (Pubitemid 350257009)
182. J.Z. Long, X. Jin, A. Adibekian, W. Li, and B.F. Cravatt Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases J. Med. Chem. 53 2010 1830 1842
183. J. Chang, M. Niphakis, K. Lum,C. Wang, M. Matthews, S. Niessen, M. Buczynski, L. Parsons, and B. Cravatt Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates Chem. Biol. 19 2012 579 588
184. N. Aaltonen, J. Savinainen, C. Ribas, J. Rönkkö, A. Kuusisto, J. Korhonen, D. Navia-Paldanius, J. Häyrinen, P. Takabe, H. Käsnänen, T. Pantsar, T. Laitinen, M. Lehtonen, S. Pasonen-Seppänen, A. Poso, T. Nevalainen, and J. Laitinen Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase Chem. Biol. 20 2013 379 390
185. J. Wang, and N. Ueda Biology of endocannabinoid synthesis system Prostaglandins Other Lipid Mediat. 89 2009 112 119
186. T. Bisogno, F. Howell, G. Williams, A. Minassi, M.G. Cascio, A. Ligresti, I. Matias, A. Schiano-Moriello, P. Paul, E.J. Williams, U. Gangadharan, C. Hobbs, V. Di Marzo, and P. Doherty Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain J. Cell Biol. 163 2003 463 468 (Pubitemid 37429860)
187. Y. Gao, D.V. Vasilyev, M.B. Goncalves, F.V. Howell, C. Hobbs, M. Reisenberg, R. Shen, M.Y. Zhang, B.W. Strassle, P. Lu, L. Mark, M.J. Piesla, K. Deng, E.V. Kouranova, R.H. Ring, G.T. Whiteside, B. Bates, F.S. Walsh, G. Williams, M.N. Pangalos, T.A. Samad, and P. Doherty Loss of retrograde endocannabinoid signaling and reduced adult neurogenesis in diacylglycerol lipase knock-out mice J. Neurosci. 30 2010 2017 2024
188. A. Tanimura, M. Yamazaki, Y. Hashimotodani, M. Uchigashima, S. Kawata, M. Abe, Y. Kita, K. Hashimoto, T. Shimizu, M. Watanabe, K. Sakimura, and M. Kano The endocannabinoid 2-arachidonoylglycerol produced by diacylglycerol lipase alpha mediates retrograde suppression of synaptic transmission Neuron 65 2010 320 327
189. K.L. Hsu, K. Tsuboi, A. Adibekian, H. Pugh, K. Masuda, and B.F. Cravatt DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses Nat. Chem. Biol. 8 2012 999 1007
190. N. Stella, P. Schweitzer, and D. Piomelli A second endogenous cannabinoid that modulates long-term potentiation Nature 388 1997 773 778 (Pubitemid 27375156)
191. T. Bisogno, M.G. Cascio, B. Saha, A. Mahadevan, P. Urbani, A. Minassi, G. Appendino, C. Saturnino, B. Martin, R. Razdan, and V. Di Marzo Development of the first potent and specific inhibitors of endocannabinoid biosynthesis Biochim. Biophys. Acta 1761 2006 205 212
192. Y. Liu, M.P. Patricelli, and B.F. Cravatt Activity-based protein profiling: the serine hydrolases Proc. Natl. Acad. Sci. U. S. A. 96 1999 14694 14699 (Pubitemid 30019702)
193. H.S. Hoover, J.L. Blankman, S. Niessen, and B.F. Cravatt Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling Bioorg. Med. Chem. Lett. 18 2008 5838 5841
194. D. Leung, C. Hardouin, D.L. Boger, and B.F. Cravatt Discovering potent and selective reversible inhibitors of enzymes in complex proteomes Nat. Biotechnol. 21 2003 687 691 (Pubitemid 36638097)
195. M.W. Lee, F.B. Kraemer, and D.L. Severson Characterization of a partially purified diacylglycerol lipase from bovine aorta Biochim. Biophys. Acta 1254 1995 311 318
196. G. Ortar, T. Bisogno, A. Ligresti, E. Morera, M. Nalli, and V. Di Marzo Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism J. Med. Chem. 51 2008 6970 6979
197. A. Adibekian, B.R. Martin, C. Wang, K.L. Hsu, D.A. Bachovchin, S. Niessen, H. Hoover, and B.F. Cravatt Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors Nat. Chem. Biol. 7 2011 469 478
198. M. Schweiger, R. Schreiber, G. Haemmerle, A. Lass, C. Fledelius, P. Jacobsen, H. Tornqvist, R. Zechner, and R. Zimmermann Adipose triglyceride lipase and hormone-sensitive lipase are the major enzymes in adipose tissue triacylglycerol catabolism J. Biol. Chem. 281 2006 40236 40241 (Pubitemid 46041828)
199. M. Vaughan, J.E. Berger, and D. Steinberg Hormone-sensitive lipase and monoglyceride lipase activities in adipose tissue J. Biol. Chem. 239 1964 401 409
200. C. Holm, T. Osterlund, H. Laurell, and J.A. Contreras Molecular mechanisms regulating hormone-sensitive lipase and lipolysis Annu. Rev. Nutr. 20 2000 365 393
201. C. Holm, T.G. Kirchgessner, K.L. Svenson, G. Fredrikson, S. Nilsson, C.G. Miller, J.E. Shively, C. Heinzmann, R.S. Sparkes, and T. Mohandas et al. Hormone-sensitive lipase: sequence, expression, and chromosomal localization to 19 cent-q13.3 Science 241 1988 1503 1506
202. L.S. Holst, D. Langin, H. Mulder, H. Laurell, J. Grober, A. Bergh, H.W. Mohrenweiser, G. Edgren, and C. Holm Molecular cloning, genomic organization, and expression of a testicular isoform of hormone-sensitive lipase Genomics 35 1996 441 447 (Pubitemid 26270009)
203. H. Mulder, L.S. Holst, H. Svensson, E. Degerman, F. Sundler, B. Ahren, P. Rorsman, and C. Holm Hormone-sensitive lipase, the rate-limiting enzyme in triglyceride hydrolysis, is expressed and active in beta-cells Diabetes 48 1999 228 232 (Pubitemid 29019380)
204. C.A. Small, M.P. Rogers, J.A. Goodacre, and S.J. Yeaman Phosphorylation and activation of hormone-sensitive lipase in isolated macrophages FEBS Lett. 279 1991 323 326
205. J.C. Khoo, K. Reue, D. Steinberg, and M.C. Schotz Expression of hormone-sensitive lipase mRNA in macrophages J. Lipid Res. 34 1993 1969 1974 (Pubitemid 23324971)
206. F.B. Kraemer, W.J. Shen, V. Natu, S. Patel, J. Osuga, S. Ishibashi, and S. Azhar Adrenal neutral cholesteryl ester hydrolase: identification, subcellular distribution, and sex differences Endocrinology 143 2002 801 806 (Pubitemid 34164028)
207. F.B. Kraemer, S. Patel, M.S. Saedi, and C. Sztalryd Detection of hormone-sensitive lipase in various tissues. I. Expression of an HSL/bacterial fusion protein and generation of anti-HSL antibodies J. Lipid Res. 34 1993 663 671 (Pubitemid 23118767)
208. S.J. Peters, D.J. Dyck, A. Bonen, and L.L. Spriet Effects of epinephrine on lipid metabolism in resting skeletal muscle Am. J. Physiol. Endocrinol. Metab. 275 1998 E300 E309
209. F.B. Kraemer, K. Tavangar, and A.R. Hoffman Developmental regulation of hormone-sensitive lipase mRNA in the rat: changes in steroidogenic tissues J. Lipid Res. 32 1991 1303 1310
210. T. Sterlund, D.J. Beussman, K. Julenius, P.H. Poon, S. Linse, J. Shabanowitz, D.F. Hunt, M.C. Schotz, Z.S. Derewenda, and C. Holm Domain identification of hormone-sensitive lipase by circular dichroism and fluorescence spectroscopy, limited proteolysis, and mass spectrometry J. Biol. Chem. 274 1999 15382 15388
211. F.B. Kraemer, and W.J. Shen Hormone-sensitive lipase: control of intracellular tri-(di-)acylglycerol and cholesteryl ester hydrolysis J. Lipid Res. 43 2002 1585 1594 (Pubitemid 35168272)
212. C. Holm Molecular mechanisms regulating hormone-sensitive lipase and lipolysis Biochem. Soc. Trans. 31 2003 1120 1124 (Pubitemid 38030921)
213. G.Y. Carmen, and S.M. Víctor Signalling mechanisms regulating lipolysis Cell. Signal. 18 2006 401 408
214. M.W. Anthonsen, L. Rönnstrand, C. Wernstedt, E. Degerman, and C. Holm Identification of novel phosphorylation sites in hormone-sensitive lipase that are phosphorylated in response to isoproterenol and govern activation properties in vitro J. Biol. Chem. 273 1998 215 221 (Pubitemid 28042196)
215. P. Belfrage, G. Fredrikson, N.O. Nilsson, and P. Stralfors Regulation of adipose tissue lipolysis: phosphorylation of hormones sensitive lipase in intact rat adipocytes FEBS Lett. 111 1980 120 124 (Pubitemid 10103780)
216. A.S. Greenberg, W.J. Shen, K. Muliro, S. Patel, S.C. Souza, R.A. Roth, and F.B. Kraemer Stimulation of lipolysis and hormone-sensitive lipase via the extracellular signal-regulated kinase pathway J. Biol. Chem. 276 2001 45456 45461
217. S.J. Yeaman Hormone-sensitive lipase - a multipurpose enzyme in lipid metabolism Biochim. Biophys. Acta 1052 1990 128 132 (Pubitemid 20113173)
218. S. Reynisdottir, M. Eriksson, B. Angelin, and P. Arner Impaired activation of adipocyte lipolysis in familial combined hyperlipidemia J. Clin. Invest. 95 1995 2161 2169
219. M. Klannemark, M. Orho, D. Langin, H. Laurell, C. Holm, S. Reynisdottir, P. Arner, and L. Groop The putative role of the hormone-sensitive lipase gene in the pathogenesis of Type II diabetes mellitus and abdominal obesity Diabetologia 41 1998 1516 1522 (Pubitemid 28551624)
220. L. Hellström, D. Langin, S. Reynisdottir, M. Dauzats, and P. Arner Adipocyte lipolysis in normal weight subjects with obesity among first-degree relatives Diabetologia 39 1996 921 928 (Pubitemid 26249111)
221. M.P. Thompson, S.T. Cooper, B.R. Parry, and J.A. Tuckey Increased expression of the mRNA for hormone-sensitive lipase in adipose tissue of cancer patients Biochim. Biophys. Acta 1180 1993 236 242 (Pubitemid 23033014)
222. C.A. Jepson, and S.J. Yeaman Inhibition of hormone-sensitive lipase by intermediary lipid metabolites FEBS Lett. 310 1992 197 200
223. J.N. Fain, and R.E. Shepherd Free fatty acids as feedback regulators of adenylate cyclase and cyclic 3′:5′-AMP accumulation in rat fat cells J. Biol. Chem. 250 1975 6586 6592
224. L. Vertesy, B. Beck, M. Bronstrup, K. Ehrlich, M. Kurz, G. Muller, D. Schummer, and G. Seibert Cyclipostins, novel hormone-sensitive lipase inhibitors from Streptomyces sp. DSM 13381. II. Isolation, structure elucidation and biological properties J. Antibiot. 55 2002 480 494 (Pubitemid 34746670)
225. Y.B. Ali, R. Verger, F. Carriere, S. Petry, G. Muller, and A. Abousalham The molecular mechanism of human hormone-sensitive lipase inhibition by substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones Biochimie 94 2012 137 145
226. D.B. Lowe, S. Magnuson, N. Qi, A.M. Campbell, J. Cook, Z. Hong, M. Wang, M. Rodriguez, F. Achebe, H. Kluender, W.C. Wong, W.H. Bullock, A.I. Salhanick, T. Witman-Jones, M.E. Bowling, C. Keiper, and K.B. Clairmont In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase Bioorg. Med. Chem. Lett. 14 2004 3155 3159 (Pubitemid 38624583)
227. T.H. Claus, D.B. Lowe, Y. Liang, A.I. Salhanick, C.K. Lubeski, L. Yang, L. Lemoine, J. Zhu, and K.B. Clairmont Specific inhibition of hormone-sensitive lipase improves lipid profile while reducing plasma glucose J. Pharmacol. Exp. Ther. 315 2005 1396 1402 (Pubitemid 41635430)
228. D.H. Slee, A.S. Bhat, T.N. Nguyen, M. Kish, K. Lundeen, M.J. Newman, and S.J. McConnell Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase J. Med. Chem. 46 2003 1120 1122 (Pubitemid 36428216)
229. J.C. de Jong, L.G. Sørensen, H. Tornqvist, and P. Jacobsen Carbazates as potent inhibitors of hormone-sensitive lipase Bioorg. Med. Chem. Lett. 14 2004 1741 1744 (Pubitemid 38340678)
230. S. Ebdrup, H.H. Refsgaard, C. Fledelius, and P. Jacobsen Synthesis and structure-activity relationship for a novel class of potent and selective carbamate-based inhibitors of hormone selective lipase with acute in vivo antilipolytic effects J. Med. Chem. 50 2007 5449 5456 (Pubitemid 350057854)
231. Y. Ben-Ali, and G. Muller Kinetic characterization and specific inhibition of hormone-sensitive lipase 46th International Conference on the Bioscience of, Lipids vol. 136 2005
232. S. Ebdrup, L.G. Sørensen, O.H. Olsen, and P. Jacobsen Synthesis and structure-activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase J. Med. Chem. 47 2004 400 410 (Pubitemid 38057883)
233. R. Zimmermann, J.G. Strauss, G. Haemmerle, G. Schoiswohl, R. Birner-Gruenberger, M. Riederer, A. Lass, G. Neuberger, F. Eisenhaber, A. Hermetter, and R. Zechner Fat mobilization in adipose tissue is promoted by adipose triglyceride lipase Science 306 2004 1383 1386 (Pubitemid 39532517)
234. J.A. Villena, S. Roy, E. Sarkadi-Nagy, K.H. Kim, and H.S. Sul Desnutrin, an adipocyte gene encoding a novel patatin domain-containing protein, is induced by fasting and glucocorticoids J. Biol. Chem. 279 2004 47066 47075
235. C.M. Jenkins, D.J. Mancuso, W. Yan, H.F. Sims, B. Gibson, and R.W. Gross Identification, cloning, expression, and purification of three novel human calcium-independent phospholipase A2 family members possessing triacylglycerol lipase and acylglycerol transacylase activities J. Biol. Chem. 279 2004 48968 48975 (Pubitemid 39625778)
236. M. Schweiger, G. Schoiswohl, A. Lass, F.P. Radner, G. Haemmerle, R. Malli, W. Graier, I. Cornaciu, M. Oberer, R. Salvayre, J. Fischer, R. Zechner, and R. Zimmermann The C-terminal region of human adipose triglyceride lipase affects enzyme activity and lipid droplet binding J. Biol. Chem. 283 2008 17211 17220
237. K. Kobayashi, T. Inoguchi, Y. Maeda, N. Nakashima, A. Kuwano, E. Eto, N. Ueno, S. Sasaki, F. Sawada, M. Fujii, Y. Matoba, S. Sumiyoshi, H. Kawate, and R. Takayanagi The lack of the C-terminal domain of adipose triglyceride lipase causes neutral lipid storage disease through impaired interactions with lipid droplets J. Clin. Endocrinol. Metab. 93 2008 2877 2884 (Pubitemid 352008564)
238. A.C. Lake, Y. Sun, J.L. Li, J.E. Kim, J.W. Johnson, D. Li, T. Revett, H.H. Shih, W. Liu, J.E. Paulsen, and R.E. Gimeno Expression, regulation, and triglyceride hydrolase activity of Adiponutrin family members J. Lipid Res. 46 2005 2477 2487 (Pubitemid 41532536)
239. M.J. Watt, B.J. van Denderen, L.A. Castelli, C.R. Bruce, A.J. Hoy, E.W. Kraegen, L. Macaulay, and B.E. Kemp Adipose triglyceride lipase regulation of skeletal muscle lipid metabolism and insulin responsiveness Mol. Endocrinol. 22 2008 1200 1212 (Pubitemid 351629619)
240. M.J. Watt, and G.R. Steinberg Regulation and function of triacylglycerol lipases in cellular metabolism Biochem. J. 414 2008 313 325
241. P.A. Wilson, S.D. Gardner, N.M. Lambie, S.A. Commans, and D.J. Crowther Characterization of the human patatin-like phospholipase family J. Lipid Res. 47 2006 1940 1949 (Pubitemid 44401981)
242. E. Smirnova, E.B. Goldberg, K.S. Makarova, L. Lin, W.J. Brown, and C.L. Jackson ATGL has a key role in lipid droplet/adiposome degradation in mammalian cells EMBO Rep. 7 2006 106 113
243. G. Haemmerle, A. Lass, R. Zimmermann, G. Gorkiewicz, C. Meyer, J. Rozman, G. Heldmaier, R. Maier, C. Theussl, S. Eder, D. Kratky, E.F. Wagner, M. Klingenspor, G. Hoefler, and R. Zechner Defective lipolysis and altered energy metabolism in mice lacking adipose triglyceride lipase Science 312 2006 734 737
244. E.E. Kershaw, J.K. Hamm, L.A. Verhagen, O. Peroni, M. Katic, and J.S. Flier Adipose triglyceride lipase: function, regulation by insulin, and comparison with adiponutrin Diabetes 55 2006 148 157 (Pubitemid 43343310)
245. A. Lass, R. Zimmermann, G. Haemmerle, M. Riederer, G. Schoiswohl, M. Schweiger, P. Kienesberger, J.G. Strauss, G. Gorkiewicz, and R. Zechner Adipose triglyceride lipase-mediated lipolysis of cellular fat stores is activated by CGI-58 and defective in Chanarin-Dorfman Syndrome Cell Metab. 3 2006 309 319
246. D.L. Brasaemle Thematic review series: adipocyte biology. The perilipin family of structural lipid droplet proteins: stabilization of lipid droplets and control of lipolysis J. Lipid Res. 48 2007 2547 2559 (Pubitemid 350272839)
247. C. Chung, J.A. Doll, A.K. Gattu, C. Shugrue, M. Cornwell, P. Fitchev, and S.E. Crawford Anti-angiogenic pigment epithelium-derived factor regulates hepatocyte triglyceride content through adipose triglyceride lipase (ATGL) J. Hepatol. 48 2008 471 478
248. R. Zimmerman, R. Zechner, G. Haemmerle, G. Hofler, S. Das, A. Lass, Modulation of adipose triglyceride lipase for prevention and treatment of cachexia, loss of weight and muscle atrophy and methods of screening thereof, US Patent 0230943, 2012.
249. N. Mayer, M. Schweiger, M. Romauch, G.F. Grabner, T.O. Eichmann, E. Fuchs, J. Ivkovic, C. Heier, I. Mrak, A. Lass, G. Hofler, C. Fledelius, R. Zechner, R. Zimmermann, and R. Breinbauer Development of small-molecule inhibitors targeting adipose triglyceride lipase Nat. Chem. Biol. 9 2013 785 787
250. V. Subramanian, A. Rothenberg, C. Gomez, A.W. Cohen, A. Garcia, S. Bhattacharyya, L. Shapiro, G. Dolios, R. Wang, M.P. Lisanti, and D.L. Brasaemle Perilipin A mediates the reversible binding of CGI-58 to lipid droplets in 3 T3-L1 adipocytes J. Biol. Chem. 279 2004 42062 42071 (Pubitemid 39313657)
251. T. Yamaguchi, N. Omatsu, S. Matsushita, and T. Osumi CGI-58 interacts with perilipin and is localized to lipid droplets. Possible involvement of CGI-58 mislocalization in Chanarin-Dorfman syndrome J. Biol. Chem. 279 2004 30490 30497 (Pubitemid 38937979)
252. D.L. Ollis, E. Cheah, M. Cygler, B. Dijkstra, F. Frolow, S.M. Franken, M. Harel, S.J. Remington, I. Silman, and J. Schrag et al. The alpha/beta hydrolase fold Protein Eng. 5 1992 197 211
253. N. Lenfant, T. Hotelier, Y. Bourne, P. Marchot, and A. Chatonnet Proteins with an alpha/beta hydrolase fold: relationships between subfamilies in an ever-growing superfamily Chem. Biol. Interact. 203 2013 266 268
254. G.M. Simon, and B.F. Cravatt Activity-based proteomics of enzyme superfamilies: serine hydrolases as a case study J. Biol. Chem. 285 2010 11051 11055
255. D. Navia-Paldanius, J.R. Savinainen, and J.T. Laitinen Biochemical and pharmacological characterization of human alpha/beta-hydrolase domain containing 6 (ABHD6) and 12 (ABHD12) J. Lipid Res. 53 2012 2413 2424
256. T. Yamaguchi, N. Omatsu, E. Morimoto, H. Nakashima, K. Ueno, T. Tanaka, K. Satouchi, F. Hirose, and T. Osumi CGI-58 facilitates lipolysis on lipid droplets but is not involved in the vesiculation of lipid droplets caused by hormonal stimulation J. Lipid Res. 48 2007 1078 1089 (Pubitemid 46708675)
257. C. Lefevre, F. Jobard, F. Caux, B. Bouadjar, A. Karaduman, R. Heilig, H. Lakhdar, A. Wollenberg, J.L. Verret, J. Weissenbach, M. Ozguc, M. Lathrop, J.F. Prud'homme, and J. Fischer Mutations in CGI-58, the gene encoding a new protein of the esterase/lipase/thioesterase subfamily, in Chanarin-Dorfman syndrome Am. J. Hum. Genet. 69 2001 1002 1012 (Pubitemid 33015815)
258. A. Gruber, I. Cornaciu, A. Lass, M. Schweiger, M. Poeschl, C. Eder, M. Kumari, G. Schoiswohl, H. Wolinski, S.D. Kohlwein, R. Zechner, R. Zimmermann, and M. Oberer The N-terminal region of comparative gene identification-58 (CGI-58) is important for lipid droplet binding and activation of adipose triglyceride lipase J. Biol. Chem. 285 2010 12289 12298
259. J.G. Granneman, H.P. Moore, R. Krishnamoorthy, and M. Rathod Perilipin controls lipolysis by regulating the interactions of AB-hydrolase containing 5 (Abhd5) and adipose triglyceride lipase (Atgl) J. Biol. Chem. 284 2009 34538 34544
260. M. Schweiger, A. Lass, R. Zimmermann, T.O. Eichmann, and R. Zechner Neutral lipid storage disease: genetic disorders caused by mutations in adipose triglyceride lipase/PNPLA2 or CGI-58/ABHD5 Am. J. Physiol. Endocrinol. Metab. 297 2009 E289 E296
261. F.P. Radner, I.E. Streith, G. Schoiswohl, M. Schweiger, M. Kumari, T.O. Eichmann, G. Rechberger, H.C. Koefeler, S. Eder, S. Schauer, H.C. Theussl, K. Preiss-Landl, A. Lass, R. Zimmermann, G. Hoefler, R. Zechner, and G. Haemmerle Growth retardation, impaired triacylglycerol catabolism, hepatic steatosis, and lethal skin barrier defect in mice lacking comparative gene identification-58 (CGI-58) J. Biol. Chem. 285 2010 7300 7311
262. J.M. Brown, J.L. Betters, C. Lord, Y. Ma, X. Han, K. Yang, H.M. Alger, J. Melchior, J. Sawyer, R. Shah, M.D. Wilson, X. Liu, M.J. Graham, R. Lee, R. Crooke, G.I. Shulman, B. Xue, H. Shi, and L. Yu CGI-58 knockdown in mice causes hepatic steatosis but prevents diet-induced obesity and glucose intolerance J. Lipid Res. 51 2010 3306 3315
263. G. Montero-Moran, J.M. Caviglia, D. McMahon, A. Rothenberg, V. Subramanian, Z. Xu, S. Lara-Gonzalez, J. Storch, G.M. Carman, and D.L. Brasaemle CGI-58/ABHD5 is a coenzyme A-dependent lysophosphatidic acid acyltransferase J. Lipid Res. 51 2010 709 719
264. A.K. Ghosh, G. Ramakrishnan, C. Chandramohan, and R. Rajasekharan CGI-58, the causative gene for Chanarin-Dorfman syndrome, mediates acylation of lysophosphatidic acid J. Biol. Chem. 283 2008 24525 24533
265. C.C. Lord, J.L. Betters, P.T. Ivanova, S.B. Milne, D.S. Myers, J. Madenspacher, G. Thomas, S. Chung, M. Liu, M.A. Davis, R.G. Lee, R.M. Crooke, M.J. Graham, J.S. Parks, D.L. Brasaemle, M.B. Fessler, H.A. Brown, and J.M. Brown CGI-58/ABHD5-derived signaling lipids regulate systemic inflammation and insulin action Diabetes 61 2012 355 363
266. T. Yamaguchi Crucial role of CGI-58/alpha/beta hydrolase domain-containing protein 5 in lipid metabolism Biol. Pharm. Bull. 33 2010 342 345
267. D.L. Andrews, B. Beames, M.D. Summers, and W.D. Park Characterization of the lipid acyl hydrolase activity of the major potato (Solanum tuberosum) tuber protein, patatin, by cloning and abundant expression in a baculovirus vector Biochem. J. 252 1988 199 206
268. P.C. Kienesberger, M. Oberer, A. Lass, and R. Zechner Mammalian patatin domain containing proteins: a family with diverse lipolytic activities involved in multiple biological functions J. Lipid Res. 50 2009 S63 S68
269. S. Baulande, F. Lasnier, M. Lucas, and J. Pairault Adiponutrin, a transmembrane protein corresponding to a novel dietary- and obesity-linked mRNA specifically expressed in the adipose lineage J. Biol. Chem. 276 2001 33336 33344
270. R.G. Victor, R.W. Haley, D.L. Willett, R.M. Peshock, P.C. Vaeth, D. Leonard, M. Basit, R.S. Cooper, V.G. Iannacchione, W.A. Visscher, J.M. Staab, and H.H. Hobbs The Dallas Heart Study: a population-based probability sample for the multidisciplinary study of ethnic differences in cardiovascular health Am. J. Cardiol. 93 2004 1473 1480 (Pubitemid 38749202)
271. S. Romeo, J. Kozlitina, C. Xing, A. Pertsemlidis, D. Cox, L.A. Pennacchio, E. Boerwinkle, J.C. Cohen, and H.H. Hobbs Genetic variation in PNPLA3 confers susceptibility to nonalcoholic fatty liver disease Nat. Genet. 40 2008 1461 1465
272. S. He, C. McPhaul, J.Z. Li, R. Garuti, L. Kinch, N.V. Grishin, J.C. Cohen, and H.H. Hobbs A sequence variation (I148M) in PNPLA3 associated with nonalcoholic fatty liver disease disrupts triglyceride hydrolysis J. Biol. Chem. 285 2010 6706 6715
273. B.N. Reid, G.P. Ables, O.A. Otlivanchik, G. Schoiswohl, R. Zechner, W.S. Blaner, I.J. Goldberg, R.F. Schwabe, S.C. Chua Jr., and L.S. Huang Hepatic overexpression of hormone-sensitive lipase and adipose triglyceride lipase promotes fatty acid oxidation, stimulates direct release of free fatty acids, and ameliorates steatosis J. Biol. Chem. 283 2008 13087 13099
274. J.D. Browning, J.C. Cohen, and H.H. Hobbs Patatin-like phospholipase domain-containing 3 and the pathogenesis and progression of pediatric nonalcoholic fatty liver disease Hepatology 52 2010 1189 1192
275. J.Z. Li, Y. Huang, R. Karaman, P.T. Ivanova, H.A. Brown, T. Roddy, J. Castro-Perez, J.C. Cohen, and H.H. Hobbs Chronic overexpression of PNPLA3I148M in mouse liver causes hepatic steatosis J. Clin. Invest. 122 2012 4130 4144
276. M. Kumari, G. Schoiswohl, C. Chitraju, M. Paar, I. Cornaciu, A.Y. Rangrez, N. Wongsiriroj, H.M. Nagy, P.T. Ivanova, S.A. Scott, O. Knittelfelder, G.N. Rechberger, R. Birner-Gruenberger, S. Eder, H.A. Brown, G. Haemmerle, M. Oberer, A. Lass, E.E. Kershaw, R. Zimmermann, and R. Zechner Adiponutrin functions as a nutritionally regulated lysophosphatidic acid acyltransferase Cell Metab. 15 2012 691 702
277. T.E. Harris, and B.N. Finck Dual function lipin proteins and glycerolipid metabolism Trends Endocrinol. Metab. 22 2011 226 233
278. E.P. Kennedy, S.W. Smith, and S.B. Weiss New synthesis of lecithin in an isolated enzyme system Nature 178 1956 594 595
279. M. Peterfy, J. Phan, P. Xu, and K. Reue Lipodystrophy in the fld mouse results from mutation of a new gene encoding a nuclear protein, lipin Nat. Genet. 27 2001 121 124 (Pubitemid 32044532)
280. J. Donkor, M. Sariahmetoglu, J. Dewald, D.N. Brindley, and K. Reue Three mammalian lipins act as phosphatidate phosphatases with distinct tissue expression patterns J. Biol. Chem. 282 2007 3450 3457 (Pubitemid 47084457)
281. C.A. Langner, E.H. Birkenmeier, O. Ben-Zeev, M.C. Schotz, H.O. Sweet, M.T. Davisson, and J.I. Gordon The fatty liver dystrophy (fld) mutation. A new mutant mouse with a developmental abnormality in triglyceride metabolism and associated tissue-specific defects in lipoprotein lipase and hepatic lipase activities J. Biol. Chem. 264 1989 7994 8003 (Pubitemid 19137280)
282. M.C. Gropler, T.E. Harris, A.M. Hall, N.E. Wolins, R.W. Gross, X. Han, Z. Chen, and B.N. Finck Lipin 2 is a liver-enriched phosphatidate phosphohydrolase enzyme that is dynamically regulated by fasting and obesity in mice J. Biol. Chem. 284 2009 6763 6772
283. T.A. Huffman, I. Mothe-Satney, and J.C. Lawrence Insulin-stimulated phosphorylation of lipin mediated by the mammalian target of rapamycin Proc. Natl. Acad. Sci. U. S. A. 99 2002 1047 1052 (Pubitemid 34106633)
284. T.E. Harris, T.A. Huffman, A. Chi, J. Shabanowitz, D.F. Hunt, A. Kumar, and J.C. Lawrence Insulin controls subcellular localization and multisite phosphorylation of the phosphatidic acid phosphatase, lipin 1 J. Biol. Chem. 282 2007 277 286 (Pubitemid 47076630)
285. B.N. Finck, M.C. Gropler, Z. Chen, T.C. Leone, M.A. Croce, T.E. Harris, J.C. Lawrence, and D.P. Kelly Lipin 1 is an inducible amplifier of the hepatic PGC-1alpha/PPARalpha regulatory pathway Cell Metab. 4 2006 199 210 (Pubitemid 44283957)
286. E. Suviolahti, K. Reue, R.M. Cantor, J. Phan, M. Gentile, J. Naukkarinen, A. Soro-Paavonen, L. Oksanen, J. Kaprio, A. Rissanen, V. Salomaa, K. Kontula, M.R. Taskinen, P. Pajukanta, and L. Peltonen Cross-species analyses implicate Lipin 1 involvement in human glucose metabolism Hum. Mol. Genet. 15 2006 377 386 (Pubitemid 43159890)
287. A. Yao-Borengasser, N. Rasouli, V. Varma, L.M. Miles, B. Phanavanh, T.N. Starks, J. Phan, H.J. Spencer, R.E. McGehee, K. Reue, and P.A. Kern Lipin expression is attenuated in adipose tissue of insulin-resistant human subjects and increases with peroxisome proliferator-activated receptor gamma activation Diabetes 55 2006 2811 2818 (Pubitemid 44923681)
288. M.A. Croce, J.C. Eagon, L.L. LaRiviere, K.M. Korenblat, S. Klein, and B.N. Finck Hepatic lipin 1beta expression is diminished in insulin-resistant obese subjects and is reactivated by marked weight loss Diabetes 56 2007 2395 2399 (Pubitemid 47358247)
289. R.A. Coleman, and D.G. Mashek Mammalian triacylglycerol metabolism: synthesis, lipolysis, and signaling Chem. Rev. 111 2011 6359 6386
290. E.P. Kennedy Biosynthesis of complex lipids Fed. Proc. 20 1961 934 940
291. L. Dircks, and H.S. Sul Acyltransferases of de novo glycerophospholipid biosynthesis Prog. Lipid Res. 38 1999 461 479
292. R.A. Coleman, and D.P. Lee Enzymes of triacylglycerol synthesis and their regulation Prog. Lipid Res. 43 2004 134 176 (Pubitemid 37492937)
293. R.E. Gimeno, and J. Cao Thematic review series: glycerolipids. Mammalian glycerol-3-phosphate acyltransferases: new genes for an old activity J. Lipid Res. 49 2008 2079 2088
294. M. Pellon-Maison, M.A. Montanaro, R.A. Coleman, and M.R. Gonzalez-Baro Mitochondrial glycerol-3-P acyltransferase 1 is most active in outer mitochondrial membrane but not in mitochondrial associated vesicles (MAV) Biochim. Biophys. Acta 1771 2007 830 838 (Pubitemid 46891298)
295. E.A. Karlsson, S. Wang, Q. Shi, R.A. Coleman, and M.A. Beck Glycerol-3-phosphate acyltransferase 1 is essential for the immune response to infection with coxsackievirus B3 in mice J. Nutr. 139 2009 779 783
296. L.E. Hammond, C.D. Albright, L. He, I. Rusyn, S.M. Watkins, S.D. Doughman, J.J. Lemasters, and R.A. Coleman Increased oxidative stress is associated with balanced increases in hepatocyte apoptosis and proliferation in glycerol-3-phosphate acyltransferase-1 deficient mice Exp. Mol. Pathol. 82 2007 210 219 (Pubitemid 46505131)
297. S. Wang, D.P. Lee, N. Gong, N.M. Schwerbrock, D.G. Mashek, M.R. Gonzalez-Baro, C. Stapleton, L.O. Li, T.M. Lewin, and R.A. Coleman Cloning and functional characterization of a novel mitochondrial N-ethylmaleimide-sensitive glycerol-3-phosphate acyltransferase (GPAT2) Arch. Biochem. Biophys. 465 2007 347 358 (Pubitemid 47361998)
298. J. Cao, J.L. Li, D. Li, J.F. Tobin, and R.E. Gimeno Molecular identification of microsomal acyl-CoA:glycerol-3-phosphate acyltransferase, a key enzyme in de novo triacylglycerol synthesis Proc. Natl. Acad. Sci. U. S. A. 103 2006 19695 19700 (Pubitemid 46037494)
299. C.A. Nagle, L. Vergnes, H. Dejong, S. Wang, T.M. Lewin, K. Reue, and R.A. Coleman Identification of a novel sn-glycerol-3-phosphate acyltransferase isoform, GPAT4, as the enzyme deficient in Agpat6 -/- mice J. Lipid Res. 49 2008 823 831
300. Y.Q. Chen, M.S. Kuo, S. Li, H.H. Bui, D.A. Peake, P.E. Sanders, S.J. Thibodeaux, S. Chu, Y.W. Qian, Y. Zhao, D.S. Bredt, D.E. Moller, R.J. Konrad, A.P. Beigneux, S.G. Young, and G. Cao AGPAT6 is a novel microsomal glycerol-3-phosphate acyltransferase J. Biol. Chem. 283 2008 10048 10057
301. A.A. Wendel, T.M. Lewin, and R.A. Coleman Glycerol-3-phosphate acyltransferases: rate limiting enzymes of triacylglycerol biosynthesis Biochim. Biophys. Acta 1791 2009 501 506
302. H. Park, V.K. Kaushik, S. Constant, M. Prentki, E. Przybytkowski, N.B. Ruderman, and A.K. Saha Coordinate regulation of malonyl-CoA decarboxylase, sn-glycerol-3-phosphate acyltransferase, and acetyl-CoA carboxylase by AMP-activated protein kinase in rat tissues in response to exercise J. Biol. Chem. 277 2002 32571 32577 (Pubitemid 34984761)
303. E.A. Wydysh, S.M. Medghalchi, A. Vadlamudi, and C.A. Townsend Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors J. Med. Chem. 52 2009 3317 3327
304. F.P. Kuhajda, S. Aja, Y. Tu, W.F. Han, S.M. Medghalchi, R. El Meskini, L.E. Landree, J.M. Peterson, K. Daniels, K. Wong, E.A. Wydysh, C.A. Townsend, and G.V. Ronnett Pharmacological glycerol-3-phosphate acyltransferase inhibition decreases food intake and adiposity and increases insulin sensitivity in diet-induced obesity Am. J. Physiol. Regul. Integr. Comp. Physiol. 301 2011 R116 R130
305. E.A. Wydysh, A. Vadlamudi, S.M. Medghalchi, and C.A. Townsend Design, synthesis, and biological evaluation of conformationally constrained glycerol 3-phosphate acyltransferase inhibitors Bioorg. Med. Chem. 18 2010 6470 6479
306. J. Kanfer, and E.P. Kennedy Metabolism and function of bacterial lipids. I. Metabolism of phospholipids in Escherichia coli B J. Biol. Chem. 238 1963 2919 2922
307. J. Kanfer, and E.P. Kennedy Metabolism and function of bacterial lipids. II. Biosynthesis of phospholipids in Escherichia coli J. Biol. Chem. 239 1964 1720 1726
308. J. West, C.K. Tompkins, N. Balantac, E. Nudelman, B. Meengs, T. White, S. Bursten, J. Coleman, A. Kumar, J.W. Singer, and D.W. Leung Cloning and expression of two human lysophosphatidic acid acyltransferase cDNAs that enhance cytokine-induced signaling responses in cells DNA Cell Biol. 16 1997 691 701 (Pubitemid 27276833)
309. D.W. Leung The structure and functions of human lysophosphatidic acid acyltransferases Front. Biosci. 6 2001 D944 D953
310. C. Eberhardt, P.W. Gray, and L.W. Tjoelker Human lysophosphatidic acid acyltransferase. cDNA cloning, expression, and localization to chromosome 9q34.3 J. Biol. Chem. 272 1997 20299 20305 (Pubitemid 27340144)
311. L. Bonham, D.W. Leung, T. White, D. Hollenback, P. Klein, J. Tulinsky, M. Coon, P. de Vries, and J.W. Singer Lysophosphatidic acid acyltransferase-beta: a novel target for induction of tumour cell apoptosis Expert Opin. Ther. Targets 7 2003 643 661 (Pubitemid 37258842)
312. M. Coon, A. Ball, J. Pound, S. Ap, D. Hollenback, T. White, J. Tulinsky, L. Bonham, D.K. Morrison, R. Finney, and J.W. Singer Inhibition of lysophosphatidic acid acyltransferase beta disrupts proliferative and survival signals in normal cells and induces apoptosis of tumor cells Mol. Cancer Ther. 2 2003 1067 1078
313. D. Hollenback, L. Bonham, L. Law, E. Rossnagle, L. Romero, H. Carew, C.K. Tompkins, D.W. Leung, J.W. Singer, and T. White Substrate specificity of lysophosphatidic acid acyltransferase beta - evidence from membrane and whole cell assays J. Lipid Res. 47 2006 593 604 (Pubitemid 43345600)
314. J.M. Pagel, C. Laugen, L. Bonham, R.C. Hackman, D.M. Hockenbery, R. Bhatt, D. Hollenback, H. Carew, J.W. Singer, and O.W. Press Induction of apoptosis using inhibitors of lysophosphatidic acid acyltransferase-beta and anti-CD20 monoclonal antibodies for treatment of human non-Hodgkin's lymphomas Clin. Cancer Res. 11 2005 4857 4866 (Pubitemid 41557206)
315. T. Hideshima, D. Chauhan, T. Hayashi, K. Podar, M. Akiyama, C. Mitsiades, M.I. N, B. Gong, L. Bonham, P. de Vries, N. Munshi, P.G. Richardson, J.W. Singer, and K.C. Anderson Antitumor activity of lysophosphatidic acid acyltransferase-beta inhibitors, a novel class of agents, in multiple myeloma Cancer Res. 63 2003 8428 8436 (Pubitemid 37549499)
316. B. Gong, F. Hong, C. Kohm, S. Jenkins, J. Tulinsky, R. Bhatt, P. De Vries, J.W. Singer, and P. Klein Synthesis, SAR, and antitumor properties of diamino-C, N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta Bioorg Med Chem Lett 14 2004 2303 2308 (Pubitemid 38481409)
317. B. Gong, F. Hong, C. Kohm, L. Bonham, and P. Klein Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta Bioorg. Med. Chem. Lett. 14 2004 1455 1459 (Pubitemid 38299428)
318. E.P. Kennedy Metabolism of lipids Annu. Rev. Biochem. 26 1957 119 148
319. R.M. Bell, and R.A. Coleman Enzymes of glycerolipid synthesis in eukaryotes Annu. Rev. Biochem. 49 1980 459 487
320. C.L. Yen, S.J. Stone, S. Koliwad, C. Harris, and R.V. Farese Jr. Thematic review series: glycerolipids. DGAT enzymes and triacylglycerol biosynthesis J. Lipid Res. 49 2008 2283 2301
321. T. Kadowaki, E. Wilder, J. Klingensmith, K. Zachary, and N. Perrimon The segment polarity gene porcupine encodes a putative multitransmembrane protein involved in Wingless processing Genes Dev. 10 1996 3116 3128 (Pubitemid 27020540)
322. K.D. Lardizabal, J.T. Mai, N.W. Wagner, A. Wyrick, T. Voelker, and D.J. Hawkins DGAT2 is a new diacylglycerol acyltransferase gene family: purification, cloning, and expression in insect cells of two polypeptides from Mortierella ramanniana with diacylglycerol acyltransferase activity J. Biol. Chem. 276 2001 38862 38869
323. M.M. Assifi, G. Suchankova, S. Constant, M. Prentki, A.K. Saha, and N.B. Ruderman AMP-activated protein kinase and coordination of hepatic fatty acid metabolism of starved/carbohydrate-refed rats Am. J. Physiol. Endocrinol. Metab. 289 2005 E794 E800
324. H.P. Haagsman, C.G. de Haas, M.J. Geelen, and L.M. van Golde Regulation of triacylglycerol synthesis in the liver: a decrease in diacylglycerol acyltransferase activity after treatment of isolated rat hepatocytes with glucagon Biochim. Biophys. Acta 664 1981 74 81 (Pubitemid 11068027)
325. H.C. Chen, S.J. Smith, Z. Ladha, D.R. Jensen, L.D. Ferreira, L.K. Pulawa, J.G. McGuire, R.E. Pitas, R.H. Eckel, and R.V. Farese Jr. Increased insulin and leptin sensitivity in mice lacking acyl CoA:diacylglycerol acyltransferase 1 J. Clin. Invest. 109 2002 1049 1055 (Pubitemid 34413589)
326. L.L. Listenberger, X. Han, S.E. Lewis, S. Cases, R.V. Farese Jr., D.S. Ory, and J.E. Schaffer Triglyceride accumulation protects against fatty acid-induced lipotoxicity Proc. Natl. Acad. Sci. U. S. A. 100 2003 3077 3082 (Pubitemid 36356542)
327. K. Yamaguchi, L. Yang, S. McCall, J. Huang, X.X. Yu, S.K. Pandey, S. Bhanot, B.P. Monia, Y.X. Li, and A.M. Diehl Inhibiting triglyceride synthesis improves hepatic steatosis but exacerbates liver damage and fibrosis in obese mice with nonalcoholic steatohepatitis Hepatology 45 2007 1366 1374 (Pubitemid 46918320)
328. S.J. Smith, S. Cases, D.R. Jensen, H.C. Chen, E. Sande, B. Tow, D.A. Sanan, J. Raber, R.H. Eckel, and R.V. Farese Obesity resistance and multiple mechanisms of triglyceride synthesis in mice lacking Dgat Nat. Genet. 25 2000 87 90 (Pubitemid 30257043)
329. S.J. Stone, H.M. Myers, S.M. Watkins, B.E. Brown, K.R. Feingold, P.M. Elias, and R.V. Farese Jr. Lipopenia and skin barrier abnormalities in DGAT2-deficient mice J. Biol. Chem. 279 2004 11767 11776 (Pubitemid 38401682)
330. H.R. Wurie, L. Buckett, and V.A. Zammit Diacylglycerol acyltransferase 2 acts upstream of diacylglycerol acyltransferase 1 and utilizes nascent diglycerides and de novo synthesized fatty acids in HepG2 cells FEBS J. 279 2012 3033 3047
331. R.L. Dow Acyl-CoA; diacylglycerol acyltransferase-1 inhibition as an approach to the treatment of type 2 diabetes R.M. Jones, D.E. Thurston, D. Rotelle, S. Guiccione, A. Martinez, D. Fox, R. Gannelin, New Therapeutic Strategies for Type2 Diabetes: Small Molecule Approaches 2012 RSC Cambridge, UK 215 249
332. D. Matsuda, and H. Tomoda DGAT inhibitors for obesity Curr. Opin. Investig. Drugs 8 2007 836 841 (Pubitemid 47511881)
333. N. Tabata, M. Ito, H. Tomoda, and S. Omura Xanthohumols, diacylglycerol acyltransferase inhibitors, from Humulus lupulus Phytochemistry 46 1997 683 687 (Pubitemid 27483829)
334. H. Tomoda, Y. Ohyama, T. Abe, N. Tabata, M. Namikoshi, Y. Yamaguchi, R. Masuma, and S. Omura Roselipins, inhibitors of diacylglycerol acyltransferase, produced by Gliocladium roseum KF-1040 J. Antibiot. 52 1999 689 694 (Pubitemid 29431314)
335. M.Y. Chung, M.C. Rho, J.S. Ko, S.Y. Ryu, K.H. Jeune, K. Kim, H.S. Lee, and Y.K. Kim In vitro inhibition of diacylglycerol acyltransferase by prenylflavonoids from Sophora flavescens Planta Med. 70 2004 258 260 (Pubitemid 38445194)
336. S.W. Lee, K. Kim, M.C. Rho, M.Y. Chung, Y.H. Kim, S. Lee, H.S. Lee, and Y.K. Kim New polyacetylenes, DGAT inhibitors from the roots of Panax ginseng Planta Med. 70 2004 197 200 (Pubitemid 38445183)
337. J.S. Ko, S.Y. Ryu, Y.S. Kim, M.Y. Chung, J.S. Kang, M.C. Rho, H.S. Lee, and Y.K. Kim Inhibitory activity of diacylglycerol acyltransferase by tanshinones from the root of Salvia miltiorrhiza Arch. Pharm. Res. 25 2002 446 448
338. A.C. Rustan, J.O. Nossen, E.N. Christiansen, and C.A. Drevon Eicosapentaenoic acid reduces hepatic synthesis and secretion of triacylglycerol by decreasing the activity of acyl-coenzyme A:1,2-diacylglycerol acyltransferase J. Lipid Res. 29 1988 1417 1426 (Pubitemid 19013036)
339. W.K. Oh, C. Lee, J.H. Seo, M.Y. Chung, L. Cui, Z.T. Fomum, J.S. Kang, and H.S. Lee Diacylglycerol acyltransferase-inhibitory compounds from Erythrina senegalensis Arch. Pharm. Res. 32 2009 43 47
340. H.R. Park, M.Y. Yoo, J.H. Seo, I.S. Kim, N.Y. Kim, J.Y. Kang, L. Cui, C.S. Lee, C.H. Lee, and H.S. Lee Sesquiterpenoids isolated from the flower buds of Tussilago farfara L. inhibit diacylglycerol acyltransferase J. Agric. Food Chem. 56 2008 10493 10497
341. S.H. Ganji, S. Tavintharan, D. Zhu, Y. Xing, V.S. Kamanna, and M.L. Kashyap Niacin noncompetitively inhibits DGAT2 but not DGAT1 activity in HepG2 cells J. Lipid Res. 45 2004 1835 1845 (Pubitemid 40990875)
342. R. Smith, A.M. Campbell, M. Coish, J. Dai, D. Lowe, S. O'Connor, N. Su, G. Wang, M. Zhang, L. Zhu, Preparation and use of aryl alkyl acid derivatives for the treatment of obesity, US Pat. 0224997 A1, 2004.
343. G. Zhao, A.J. Souers, M. Voorbach, H.D. Falls, B. Droz, S. Brodjian, Y.Y. Lau, R.R. Iyengar, J. Gao, A.S. Judd, S.H. Wagaw, M.M. Ravn, K.M. Engstrom, J.K. Lynch, M.M. Mulhern, J. Freeman, B.D. Dayton, X. Wang, N. Grihalde, D. Fry, D.W. Beno, K.C. Marsh, Z. Su, G.J. Diaz, C.A. Collins, H. Sham, R.M. Reilly, M.E. Brune, and P.R. Kym Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor J. Med. Chem. 51 2008 380 383 (Pubitemid 351252263)
344. B. Fox, N. Furukawa, X. Hao, K. Ilo, T. Inaba, S. Jackson, F. Kayser, Fused bicyclic nitrogen containing heterocycles, WO Pat. 047755, 2004.
345. B.M. Fox, K. Iio, K. Li, R. Choi, T. Inaba, S. Jackson, S. Sagawa, B. Shan, M. Tanaka, A. Yoshida, and F. Kayser Discovery of pyrrolopyridazines as novel DGAT1 inhibitors Bioorg. Med. Chem. Lett. 20 2010 6030 6033
346. R.L. Dow, M.J. Munchhoff, 4-Amino-7,8-dihydropyrido[4,3-D]pyrimidin-5(6H) -one derivatives, US Pat. 0197590 A1, 2010.
347. J.G. Barlind, U.A. Bauer, A.M. Birch, S. Birtles, L.K. Buckett, R.J. Butlin, R.D. Davies, J.W. Eriksson, C.D. Hammond, R. Hovland, P. Johannesson, M.J. Johansson, P.D. Kemmitt, B.T. Lindmark, P. Morentin Gutierrez, T.A. Noeske, A. Nordin, C.J. O'Donnell, A.U. Petersson, A. Redzic, A.V. Turnbull, and J. Vinblad Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687) J. Med. Chem. 55 2012 10610 10629
348. A.M. Birch, S. Pal, A. Pettersen, G.P. Tomkinson, 1,3,4-Oxadiazole derivatives and their uses to treat diabetes, WO Pat. 070343,2010.
349. W. McCoull, M.S. Addie, A.M. Birch, S. Birtles, L.K. Buckett, R.J. Butlin, S.S. Bowker, S. Boyd, S. Chapman, R.D. Davies, C.S. Donald, C.P. Green, C. Jenner, P.D. Kemmitt, A.G. Leach, G.C. Moody, P.M. Gutierrez, N.J. Newcombe, T. Nowak, M.J. Packer, A.T. Plowright, J. Revill, P. Schofield, C. Sheldon, S. Stokes, A.V. Turnbull, S.J. Wang, D.P. Whalley, and J.M. Wood Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes Bioorg. Med. Chem. Lett. 22 2012 3873 3878
350. Y. Huang, C. Sun, M.R. Lawrence, W.R. Ewing, H. Turdi, Triazolo compounds useful as DGAT1 inhibitors, WO Pat.126624, 2009.
351. Y. Qian, S.J. Wertheimer, M. Ahmad, A.W. Cheung, F. Firooznia, M.M. Hamilton, S. Hayden, S. Li, N. Marcopulos, L. McDermott, J. Tan, W. Yun, L. Guo, A. Pamidimukkala, Y. Chen, K.S. Huang, G.B. Ramsey, T. Whittard, K. Conde-Knape, R. Taub, C.M. Rondinone, J. Tilley, and D. Bolin Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole- 4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes J. Med. Chem. 54 2011 2433 2446
352. P. Mougenot, C. Namane, E. Fett, F. Camy, R. Dadji-Faihun, G. Langot, C. Monseau, B. Onofri, F. Pacquet, C. Pascal, O. Crespin, M. Ben-Hassine, J.L. Ragot, T. Van-Pham, C. Philippo, F. Chatelain-Egger, P. Peron, J.C. Le Bail, E. Guillot, P. Chamiot-Clerc, M.A. Chabanaud, M.P. Pruniaux, F. Schmidt, O. Venier, E. Nicolai, and F. Viviani Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1 Bioorg. Med. Chem. Lett. 22 2012 2497 2502
353. U. Bali, O. Barba, G. Dawson, W.T. Gattrell, J.G. Horswill, D.A. Pan, M.J. Procter, C.M. Rasamison, C.P. Sambrook Smith, A. Taylor-Warne, and P. Wong-Kai-In Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability Bioorg. Med. Chem. Lett. 22 2012 824 828
354. K. Lee, J.I. Goo, H.Y. Jung, M. Kim, S.K. Boovanahalli, H.R. Park, M.O. Kim, D.H. Kim, H.S. Lee, and Y. Choi Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors Bioorg. Med. Chem. Lett. 22 2012 7456 7460
355. H. Motiwala, S. Kandre, V. Birar, K.S. Kadam, A. Rodge, R.D. Jadhav, and M. Mahesh Kumar Reddy, M.K. Brahma, N.J. Deshmukh, A. Dixit, L. Doshi, A. Gupte, A.K. Gangopadhyay, R.A. Vishwakarma, S. Srinivasan, M. Sharma, K.V. Nemmani, R. Sharma, Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors Bioorg. Med. Chem. Lett. 21 2011 5812 5817
356. R.D. Jadhav, K.S. Kadam, S. Kandre, T. Guha, M.M. Reddy, M.K. Brahma, N.J. Deshmukh, A. Dixit, L. Doshi, N. Potdar, A.A. Enose, R.A. Vishwakarma, H. Sivaramakrishnan, S. Srinivasan, K.V. Nemmani, A. Gupte, A.K. Gangopadhyay, and R. Sharma Synthesis and biological evaluation of isoxazole, oxazole, and oxadiazole containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors Eur. J. Med. Chem. 54 2012 324 342
357. K.S. Kadam, R.D. Jadhav, S. Kandre, T. Guha, M.M. Reddy, M.K. Brahma, N.J. Deshmukh, A. Dixit, L. Doshi, S. Srinivasan, J. Devle, A. Damre, K.V. Nemmani, A. Gupte, and R. Sharma Evaluation of thiazole containing biaryl analogs as diacylglycerol acyltransferase 1 (DGAT1) inhibitors Eur. J. Med. Chem. 65 2013 337 347
358. Y. Nakada, T.D. Aicher, Y. Le Huerou, T. Turner, S.A. Pratt, S.S. Gonzales, S.A. Boyd, H. Miki, T. Yamamoto, H. Yamaguchi, K. Kato, and S. Kitamura Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives Bioorg. Med. Chem. 18 2010 2785 2795
359. Serano-Wu, M. H., Kwan, Y. S., and Liu, W. (2007) New compounds. WO Pat. 126957 A2, 2007.