Nuclear Hormone Receptor Modulators for the Treatment of Diabetes and Dyslipidemia

Annual Reports in Medicinal Chemistry

Volumn 41, Issue , 2006, Pages 99-126

  Meinke, Peter T ^a   Wood, Harold B ^a   Szewczyk, Jason W ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 33846405252     PISSN: 00657743     EISSN: None     Source Type: Book Series    
DOI: 10.1016/S0065-7743(06)41006-X     Document Type: Review

References (179)

1. Rangwala S.M., and Lazar M.A. Trends Pharmacol. Sci. 25 (2004) 331
2. Berger J., and Moller D.E. Ann. Rev. Med. 53 (2002) 409
3. Sternbach D. Ann. Rep. Med. Chem. 38 (2003) 71
4. Willson T.M., Brown P.J., Sternbach D.D., and Henke B.R. J. Med. Chem. 43 (2000) 527
5. Guan H.P., Li Y., Jensen M.V., Newgard C.B., Steppan C.M., and Lazar M.A. Nat. Med. 8 (2002) 1122
6. Tontonoz P., Hu E., and Spiegelman B.M. Cell 79 (1994) 1147
7. Goldfine A.B., Crunkhorn S., Costello M., Gami H., Landaker E.J., Niinobe M., Yoshikawa K., Lo D., Warren A., Jimenez-Chillaron J., and Patti M.E. Diabetes 55 (2006) 640
8. Guan Y., Hao C., Cha D.R., Rao R., Lu W., Kohan D.E., Magnuson M.A., Redha R., Zhang Y., and Breyer M.D. Nat. Med. 11 (2005) 861
9. Zhang H., Zhang A., Kohan D.E., Nelson R.D., Gonzalez F.J., and Yang T. Proc. Natl. Acad. Sci. USA 102 (2005) 9406
10. Goldberg R.B., Kendall D.M., Deeg M.A., Buse J.B., Zagar A.J., Pinaire J.A., Tan M.H., Khan M.A., Perez A.T., and Jacober S.J. GLAI Study Investigators. Diabetes Care 28 (2005) 1547
11. Home P.D., Pocock S.J., Beck-Nielsen H., Gomis R., Hanefeld M., Dargie H., Komajda M., Gubb J., Biswas N., and Jones N.P. Diabetologia 8 (2005) 1726
12. Dormandy J.A., Charbonnel B., Eckland D.J., Erdmann E., Massi-Benedetti M., Moules I.K., Skene A.M., Tan M.H., Lefebvre P.J., Murray G.D., Standl E., Wilcox R.G., Wilhelmsen L., Betteridge J., Birkeland K., Golay R.J., Heine L., Koranyi M., Laakso M., Mokan A., Norkus V., Pirags T., Podar A., Scheen W., Scherbaum G., Schernthaner O., Schmitz J., Skrha U., and Smith J. Taton and PROactive investigators. Lancet 366 (2005) 1279
13. Xiang A.H., Peters R.K., Kjos S.L., Marroquin A., Goico J., Ochoa C., Kawakubo M., and Buchanan T.A. Diabetes 55 (2006) 517
14. Schopfer F.J., Lin Y., Baker P.R., Cui T., Garcia-Barrio M., Zhang J., Chen K., Chen Y.E., and Freeman B.A. Proc. Natl. Acad. Sci. USA 102 (2005) 2340
15. Baker P.R., Lin Y., Schopfer F.J., Woodcock S.R., Groeger A.L., Batthyany C., Sweeney S., Long M.H., Iles K.E., Baker L.M., Branchaud B.P., Chen Y.E., and Freeman B.A. J. Biol. Chem. 280 (2005) 42464
16. Lee H.W., Kim B.Y., Ahn J.B., Kang S.K., Lee J.H., Shin J.S., Ahn S.K., Lee S.J., and Yoon S.S. Eur. J. Med. Chem. 40 (2005) 862
17. Rybczynski P.J., Zeck R.E., Dudash Jr. J., Combs D.W., Burris T.P., Yang M., C Osborne M., Chen X., and T Demarest K. J. Med. Chem. 47 (2004) 196
18. Rybczynski P.J., Zeck R.E., Combs D.W., Turchi I., Burris T.P., Xu J.Z., Yang M., and Demarest K.T. Bioorg. Med. Chem. Lett. 13 (2003) 2359
19. Sharon A., Pratap R., Vatsyayan R., Maulik P.R., Roy U., Goel A., and Ram V.J. Bioorg. Med. Chem. Lett. 15 (2005) 3356
20. Sauerberg P., Mogensen J.P., Jeppesen L., Svensson L.A., Fleckner J., Nehlin J., Wulff E.M., and Pettersson I. Bioorg. Med. Chem. Lett. 15 (2005) 1497
21. Breidert T., Callebert J., Heneka M.T., Landreth G., Launay J.M., and Hirsch E.C. J. Neurochem. 82 (2002) 615
22. Klotz L., Schmidt M., Giese T., Sastre M., Knolle P., Klockgether T., and Heneka M.T. J. Immunol. 175 (2005) 4948
23. Watson G.S., Cholerton B.A., Reger M.A., Baker L.D., Plymate S.R., Asthana S., Fishel M.A., Kulstad J.J., Green P.S., Cook D.G., Kahn S.E., Keeling M.L., and Craft S. Am. J. Geriatr. Psychiatry 13 (2005) 950
24. Risner M.E., Saunders A.M., Altman J.F., Ormandy G.C., Craft S., Foley I.M., Zvartau-Hind M.E., Hosford D.A., and Roses A.D. Pharmacogenom. J. 6 (2006) 246
25. Watson G.S., and Craft S. CNS Drugs 17 (2003) 27
26. Kersten S., Seydoux J., Peters J.M., Gonzalez F.J., Desvergne B., and Wahli W. J. Clin. Invest. 103 (1999) 1489
27. Linton M.F., and Fazio S. Curr. Atheroscler. Rep. 2 (2000) 29
28. Rubins H.B., Robins S.J., Collins D., Fye C.L., Anderson J.W., Elam M.B., Faas F.H., Linares E., Schaefer E.J., Schectman G., Wilt T.J., and Wittes J. N. Engl. J. Med. 341 (1999) 410
29. Keech A., Simes R.J., Barter P., Best J., Scott R., Taskinen M.R., Forder P., Pillai A., Davis T., Glasziou P., Drury P., Kesaniemi Y.A., Sullivan D., Hunt D., Colman P., d'Emden M., Whiting M., Ehnholm C., and Laakso M. FIELD Study Investigators. Lancet 366 (2005) 1849
30. Tenenbaum A., Motro M., Fisman E.Z., Tanne D., Boyko V., and Behar S. Arch. Intern. Med. 165 (2005) 1154
31. Li Z., Liao C., Ko B.C., Shan S., Tong E.H., Yin Z., Pan D., Wong V.K., Shi L., Ning Z.Q., Hu W., Zhou J., Chung S.S., and Lu X.P. Bioorg. Med. Chem. Lett. 14 (2004) 3507
32. Liu K., Xu L., Berger J.P., Macnaul K.L., Zhou G., Doebber T.W., Forrest M.J., Moller D.E., and Jones A.B. J. Med. Chem. 48 (2005) 2262
33. Koyama H., Boueres J.K., Miller D.J., Berger J.P., MacNaul K.L., Wang P.R., Ippolito M.C., Wright S.D., Moller D.E., and Sahoo S.P. Bioorg. Med. Chem. Lett. 15 (2005) 3347
34. Sauerberg P., Bury P.S., Mogensen J.P., Deussen H.J., Pettersson I., Fleckner J., Nehlin J., Frederiksen K.S., Albrektsen T., Din N., Svensson L.A., Ynddal L., Wulff E.M., and Jeppesen L. J. Med. Chem. 46 (2003) 4883
35. Johnson T.E., Zhang X., Shi S., and Umbenhauer D.R. Toxicol. Appl. Pharmacol. 208 (2005) 210
36. Thomssen R., Bonk S., Propfe C., Heermann K.H., Kochel H.G., and Uy A. Med. Microbiol. Immunol. (Berl .) 181 (1992) 293
37. Dharancy S., Malapel M., Perlemuter G., Roskams T., Cheng Y., Dubuquoy L., Podevin P., Conti F., Canva V., Philippe D., Gambiez L., Mathurin P., Paris J.C., Schoonjans K., Calmus Y., Pol S., Auwerx J., and Desreumaux P. Gastroenterology 128 (2005) 334
38. Fujita N., Kaito M., Tanaka H., Horiike S., and Adachi Y. Am. J. Gastroenterol. 99 (2004) 2280
39. Kim D.J., Bility M.T., Billin A.N., Willson T.M., Gonzalez F.J., and Peters J.M. Cell Death Differ 13 (2006) 53
40. Stephen R.L., Gustafsson M.C., Jarvis M., Tatoud R., Marshall B.R., Knight D., Ehrenborg E., Harris A.L., Wolf C.R., and Palmer C.N. Cancer Res. 64 (2004) 3162
41. Gupta R.A., Wang D., Katkuri S., Wang H., Dey S.K., and DuBois R.N. Nat. Med. 10 (2004) 245
42. Yin Y., Russell R.G., Dettin L.E., Bai R., Wei Z.L., Kozikowski A.P., Kopelovich L., and Glazer R.I. Cancer Res. 65 (2005) 3950
43. Barak Y., Liao D., He W., Ong E.S., Nelson M.C., Olefsky J.M., Boland R., and Evans R.M. Proc. Natl. Acad. Sci. USA 99 (2002) 303
44. Tanaka T., Yamamoto J., Iwasaki S., Asaba H., Hamura H., Ikeda Y., Watanabe M., Magoori K., Ioka R.X., Tachibana K., Watanabe Y., Uchiyama Y., Sumi K., Iguchi H., Ito S., Doi T., Hamakubo T., Naito M., Auwerx J., Yanagisawa M., Kodama T., and Sakai J. Proc. Natl. Acad. Sci. USA 100 (2003) 15924
45. Sznaidman M.L., Haffner C.D., Maloney P.R., Fivush A., Chao E., Goreham D., Sierra M.L., LeGrumelec C., Xu H.E., Montana V.G., Lambert M.H., Willson T.M., Oliver Jr W.R., and Sternbach D.D. Bioorg. Med. Chem. Lett. 13 (2003) 1517
46. Wallace J.M., Schwarz M., Coward P., Houze J., Sawyer J.K., Kelley K.L., Chai A., and Rudel L.L. J. Lipid Res. 46 (2005) 1009
47. Weigand S., Bischoff H., Dittrich-Wengenroth E., Heckroth H., Lang D., Vaupel A., and Woltering M. Bioorg. Med. Chem. Lett. 15 (2005) 4619
48. Graham T.L., Mookherjee C., Suckling K.E., Palmer C.N., and Patel L. Atherosclerosis 181 (2005) 29
49. Jr. Oliver W.R., Shenk J.L., Snaith M.R., Russell C.S., Plunket K.D., Bodkin N.L., Lewis M.C., Winegar D.A., Sznaidman M.L., Lambert M.H., Xu H.E., Sternbach D.D., Kliewer S.A., Hansen B.C., and Willson T.M. Proc. Natl. Acad. Sci. USA 98 (2001) 5306
50. Barish G.D., Narkar V.A., and Evans R.M. J. Clin. Invest. 116 (2006) 590
51. Li A.C., Binder C.J., Gutierrez A., Brown K.K., Plotkin C.R., Pattison J.W., Valledor A.F., Davis R.A., Willson T.M., Witztum J.L., Palinski W., and Glass C.K. J. Clin. Invest. 114 (2004) 1564
52. Sprecher D.L., Johnson A., Pearce G., Watts G., and Barrett H. Circulation 112 suppl., Abs (2005) 1211
53. Seber S., Ucak S., Basat O., and Altuntas Y. Diabetes Res. Clin. Pract. 71 (2006) 52
54. Guerre-Millo M., Gervois P., Raspe E., Madsen L., Poulain P., Derudas B., Herbert J.M., Winegar D.A., Willson T.M., Fruchart J.C., Berge R.K., and Staels B. J. Biol. Chem. 275 (2000) 16638
55. Ye J.M., Doyle P.J., Iglesias M.A., Watson D.G., Cooney G.J., and Kraegen E.W. Diabetes 50 (2001) 411
56. Guo Q., Sahoo S.P., Wang P.R., Milot D.P., Ippolito M.C., Wu M.S., Baffic J., Biswas C., Hernandez M., Lam M., Sharma N., Han W., Kelly L.J., MacNaul K.L., Zhou G., Desai R., Heck J.V., Doebber T.W., Berger J.P., Moller D.E., Sparrow C.P., Chao Y.S., and Wright S.D. Endocrinology 145 (2004) 1640
57. Nomura M., Kinoshita S., Satoh H., Maeda T., Murakami K., Tsunoda M., Miyachi H., and Awano K. Bioorg. Med. Chem. Lett. 9 (1999) 533
58. Doebber T.W., Kelly L.J., Zhou G., Meurer R., Biswas C., Li Y., Wu M.S., Ippolito M.C., Chao Y.-S., Wang P.-R., Wright S.D., Moller D.E., and Berger J.P. Biochem. Biophys. Res. Commun. 318 (2004) 323
59. Decochez K., Rippley R.K., Miller J.L., De Smet M., Yan K.X., Matthijs Z., Riffel K.A., Song H., Zhu H., Maynor H.O., Tanaka W., Johnson-Levonas A.O., Davies M.J., Gottesdiener K.M., Keymeulen B., and Wagner J.A. Drugs R. D. 7 (2006) 99
60. Chakrabarti R., Vikramadithyan R.K., Misra P., Hiriyan J., Raichur S., Damarla R.K., Gershome C., Suresh J., and Rajagopalan R. Br. J. Pharmacol. 140 (2003) 527
61. Pickavance L.C., Brand C.L., Wassermann K., and Wilding J.P.H. Br. J. Pharmacol. 144 (2005) 308
62. Saad M.F., Greco S., Osei K., Lewin A.J., Edwards C., Nunez M., and Reinhardt R.R. Ragaglitazar Dose-Ranging Study Group. Diabetes Care 27 (2004) 1324
63. Devasthale P.V., Chen S., Jeon Y., Qu F., Shao C., Wang W., Zhang H., Cap M., Farrelly D., Golla R., Grover G., Harrity T., Ma Z., Moore L., Ren J., Seethala R., Cheng L., Sleph P., Sun W., Tieman A., Wetterau J.R., Doweyko A., Chandrasena G., Chang S.Y., Humphreys W.G., Sasseville V.G., Biller S.A., Ryono D.E., Selan F., Hariharan N., and Cheng P.T. J. Med. Chem. 48 (2005) 2248
64. Buse J.B., Rubin C.J., Frederich R., Viraswami-Appanna K., Lin K.C., Montoro R., Shockey G., and Davidson J.A. Clin. Ther. 27 (2005) 1181
65. Martin J.A., Brooks D.A., Prieto L., Gonzalez R., Torrado A., Rojo I., Lopez de Uralde B., Lamas C., Ferritto R., Dolores Martin-Ortega M., Agejas J., Parra F., Rizzo J.R., Rhodes G.A., Robey R.L., Alt C.A., Wendel S.R., Zhang T.Y., Reifel-Miller A., Montrose-Rafizadeh C., Brozinick J.T., Hawkins E., Misener E.A., Briere D.A., Ardecky R., Fraser J.D., and Warshawsky A.M. Bioorg. Med.Chem. Lett. 15 (2005) 51
66. M. Prince, K. Spicer, J. Caro, E. Abu-Raddad, R. Konrad, M.-D. Wang, A. Negro-Vilar and J. Dananberg, 64th Scientific Sessions of the American Diabetes Association, Orlando, FL, June 4-8, 2004, Abstract 139 OR.
67. Cronet P., Petersen J.F., Folmer R., Blomberg N., Sjoblom K., Karlsson U., Lindstedt E.L., and Bamberg K. Structure 9 (2001) 699
68. Fagerberg B., Edwards S., Halmos T., Lopatynski J., Schuster H., Stender S., Stoa-Birketvedt G., Tonstad S., Halldorsdottir S., and Gause-Nilsson I. Diabetologia 48 (2005) 1716
69. Desai R.C., Han W., Metzger E.J., Bergman J.P., Gratale D.F., MacNaul K.L., Berger J.P., Doebber T.W., Leung K., Moller D.E., Heck J.V., and Sahoo S.P. Bioorg. Med.Chem. Lett. 13 (2003) 2795
70. Desai R.C., Gratale D.F., Han W., Koyama H., Metzger E., Lombardo V.K., MacNaul K.L., Doebber T.W., Berger J.P., Leung K., Franklin R., Moller D.E., Heck J.V., and Sahoo S.P. Bioorg. Med. Chem. Lett. 13 (2003) 3541
71. Caijo F., Mosset P., Gree R., Audinot-Bouchez V., Boutin J., Renard P., Caignard D.H., and Dacquet C. Bioorg. Med. Chem. Lett. 15 (2005) 4421
72. Kliewer S.A., Sundseth S.S., Jones S.A., Brown P.J., Wisely G.B., Koble C.S., Devchand P., Wahli W., Willson T.M., Lenhard J.M., and Lehmann J.M. Proc. Natl. Acad. Sci. USA 94 (1997) 4318
73. Koyama H., Miller D.J., Boueres J.K., Desai R.C., Jones A.B., Berger J.P., MacNaul K.L., Kelly L.J., Doebber T.W., Wu M.S., Zhou G., Wang P.R., Ippolito M.C., Chao Y.S., Agrawal A.K., Franklin R., Heck J.V., Wright S.D., Moller D.E., and Sahoo S.P. J. Med. Chem. 47 (2004) 3255
74. Cai Z., Feng J., Guo Y., Li P., Shen Z., Chu F., and Guo Z. Bioorg. Med. Chem. 14 (2006) 866
75. Lowe D.B., Bifulco N., Bullock W.H., Claus T., Coish P., Dai M., Dela Cruz F.E., Dickson D., Fan D., Hoover-Litty H., Li T., Ma X., Mannelly G., Monahan M.K., Muegge I., O'Connor S., Rodriguez M., Shelekhin T., Stolle A., Sweet L., Wang M., Wang Y., Zhang C., Zhang H.J., Zhang M., Zhao K., Zhao Q., Zhu J., Zhu L., and Tsutsumi M. Bioorg. Med. Chem. Lett. 16 (2006) 297
76. Shi G.Q., Dropinski J.D., McKeever B.M., Xu S., Becker J.W., Berger J.P., MacNaul K.L., Elbrecht A., Zhou G., Doebber T.W., Wang P., Chao Y.-S., Forrest M., Heck J.V., Moller D.E., and B Jones A. J. Med. Chem. 48 (2005) 4457
77. Adams A.D., Hu Z., von Langen D., Dadiz A., Elbrecht A., MacNaul K.L., Berger J.P., Zhou G., Doebber T.W., Meurer R., Forrest M.J., Moller D.E., and Jones A.B. Bioorg. Med. Chem. Lett. 13 (2003) 3185
78. Kasuga J., Makishima M., Hashimoto Y., and Miyachi H. Bioorg. Med. Chem. Lett. 16 (2006) 554
79. Mahindroo N., Wang C.C., Liao C.C., Huang C.F., Lu I.L., Lien T.W., Peng Y.H., Huang W.J., Lin Y.T., Hsu M.C., Lin C.H., Tsai C.H., Hsu J.T., Chen X., Lyu P.C., Chao Y.S., Wu S.Y., and Hsieh H.P. J. Med. Chem. 49 (2006) 1212
80. Mahindroo N., Huang C.F., Peng Y.H., Wang C.C., Liao C.C., Lien T.W., Chittimalla S.K., Huang W.J., Chai C.H., Prakash E., Chen C.P., Hsu T.A., Peng C.H., Lu I.L., Lee L.H., Chang Y.W., Chen W.C., Chou Y.C., Chen C.T., Goparaju C.M., Chen Y.S., Lan S.J., Yu M.C., Chen X., Chao Y.S., Wu S.Y., and Hsieh H.P. J. Med.Chem. 48 (2005) 8194
81. Mogensen J.P., Jeppesen L., Bury P.S., Pettersson I., Fleckner J., Nehlin J., Frederiksen K.S., Albrektsen T., Din N., Mortensen S.B., Svensson L.A., Wassermann K., Wulff E.M., Ynddal L., and Sauerberg P. Bioorg. Med. Chem. Lett. 13 2 (2003) 257
82. Liu K.G., Smith J.S., Ayscue A.H., Henke B.R., Lambert M.H., Leesnitzer L.M., Plunket K.D., Willson T.M., and Sternbach D.D. Bioorg. Med. Chem. Lett. 11 (2001) 2385
83. Z. Zhao, X. Chen, J. Wang, H. Sun and J. S.-C. Liang, WO Patent 05080340 A1, 2005.
84. Rosenstock J., Floras-Losano F., Schwartz S., Gonzalez-Galvez G., and Karpf D.B. Diabetes 54 (2005) A11 Abstract 44-OR
85. Minoura H., Takeshita S., Ita M., Hirosumi J., Mabuchi M., Kawamura I., Nakajima S., Nakayama O., Kayakiri H., Oku T., Ohkubo-Suzuki A., Fukagawa M., Kojo H., Hanioka K., Yamasaki N., Imoto T., Kobayashi Y., and Mutoh S. Eur. J. Pharmacol. 494 (2004) 273
86. Fujimura T., Sakuma H., Konishi S., Oe T., Hosogai N., Kimura C., Aramori I., and Mutoh S. J. Pharmacol. Sci. 99 (2005) 342
87. Fujimura T., Sakuma H., Ohkubo-Suzuki A., Aramori I., and Mutoh S. Biol. Pharm. Bull. 29 (2006) 423
88. L. R. McGee, J. B. Houze, S. M. Rubenstein, A. Hagiwara, N. Furukawa and H. Shinkai, WO Patent 0200633, 2002.
89. K. Kersey, L. C. Floren, B. Pendleton, M. J. Stemien, J. Buchanon and F. Dunn, 64th ADA Scientific Sessions, Orlando, FL, 2004, Abstract 656-P.
90. Schupp M., Clemenz M., Gineste R., Witt H., Janke J., Helleboid S., Hennuyer N., Ruiz P., Unger T., Staels B., and Kintscher U. Diabetes 54 (2005) 3442
91. Benson S.C., Pershadsingh H.A., Ho C.I., Chittiboyina A., Desai P., Pravenec M., Qi N., Wang J., Avery M.A., and Kurtz T.W. Hypertension 43 (2004) 993
92. Clasen R., Schupp M., Foryst-Ludwig A., Sprang C., Clemenz M., Krikov M., Thone-Reineke C., Unger T., and Kintscher U. Hypertension 46 (2005) 137
93. Pershadsingh H.A., and Kurtz T.W. Diabetes Care 27 (2004) 1015
94. Miura Y., Yamamoto N., Tsunekawa S., Taguchi S., Eguchi Y., Ozaki N., and Oiso Y. Diabetes Care 28 (2005) 757
95. Berger J.P., Petro A.E., Macnaul K.L., Kelly L.J., Zhang B.B., Richards K., Elbrecht A., Johnson B.A., Zhou G., Doebber T.W., Biswas C., Parikh M., Sharma N., Tanen M.R., Thompson G.M., Ventre J., Adams A.D., Mosley R., Surwit R.S., and Moller D.E. Mol. Endocrinol. 17 (2003) 662
96. Dropinski J.F., Akiyama T., Einstein M., Habulihaz B., Doebber T., Berger J.P., Meinke P.T., and Shi G.Q. Bioorg. Med. Chem. Lett. 15 (2005) 5035
97. Misra P., Chakrabarti R., Vikramadithyan R.K., Bolusu G., Juluri S., Hiriyan J., Gershome C., Rajjak A., Kashireddy P., Yu S., Surapureddi S., Qi C., Zhu Y.J., Reddy M.J.K., and Ramanujam R. J. Pharmacol. Exp. Ther. 306 (2003) 763
98. Vikramadithyan R.K., Chakrabarti R., Misra P., Premkumar M., Kumar S.K., Rao C.S., Ghosh A., Reddy K.N., Uma C., and Rajagopalan R. Metabolism 49 (2000) 1417
99. Thor M., Beierlein K., Dykes G., Gustavsson A.L., Heidrich J., Jendeberg L., Lindqvist B., Pegurier C., Roussel P., Slater M., Svensson S., Sydow-Backman M., Thornstrom U., and Uppenberg J. Bioorg. Med. Chem. Lett. 12 (2002) 3565
100. Ostberg T., Svensson S., Selen G., Uppenberg J., Thor M., Sundbom M., Sydow-Backman M., Gustavsson L A., and Jendeberg L. J. Biol. Chem. 279 (2004) 41124
101. Acton 3rd J.J., Black R.M., Jones A.B., Moller D.E., Colwell L., Doebber T.W., Macnaul K.L., Berger J., and Wood H.B. Bioorg. Med. Chem. Lett. 15 (2005) 357
102. Liu K., Black R.M., Acton 3rd J.J., Mosley R., Debenham S., Abola R., Yang M., Tschirret-Guth R., Colwell L., Liu C., Wu M., Wang C.F., MacNaul K.L., McCann M.E., Moller D.E., Berger J.P., Meinke P.T., Jones A.B., and Wood H.B. Bioorg. Med. Chem. Lett. 15 (2005) 2437
103. Dey D., Medicherla S., Neogi P., Gowri M., Cheng J., Gross C., Sharma S.D., Reaven G.M., and Nag B. Metabolism 52 (2003) 1012
104. J. Huck, R. Saladin and M. Sierra, WO Patent 043951 A1, 2004.
105. Schulmann I.G. Handbook Exp. Pharmocol. 139 (1999) 215
106. Stumvoll M., and Haring H. Horm. Res. 55 (2001) 3
107. Michellys P.Y., Boehm M.F., Chen J.H., Grese T.A., Karanewsky D.S., Leibowitz M.D., Liu S., Mais D.A., Mapes C.M., Reifel-Miller A., Ogilvie K.M., Rungta D., Thompson A.W., Tyhonas J.S., Yumibe N., and Ardecky R.J. Bioorg. Med. Chem. Lett. 13 (2003) 4071
108. Michellys P.Y., D'Arrigo J., Grese T.A., Karanewsky D.S., Leibowitz M.D., Mais D.A., Mapes C.M., Reifel-Miller A., Rungta D., and Boehm M.F. Bioorg. Med. Chem. Lett. 14 (2004) 1593
109. Gernert D.L., Neel D.A., Boehm M.F., Leibowitz M.D., Mais D.A., Michellys P.Y., Rungta A., Reifel-Miller A., and Grese T.A. Bioorg. Med. Chem. Lett. 14 (2004) 2759
110. Nuclear Receptor Nomenclature Committee, Cell, 1999.
111. Tontonoz P., and Mangelsdorf D.J. Mol. Endocrinol. 17 (2003) 985
112. Attie A.D., Kastelein J.P., and Hayden M.R. J. Lipid Res. 42 (2001) 1717
113. Hubacek J.A., Berge K.E., Cohen J.C., and Hobbs H.H. Hum. Mutat. 18 (2001) 359
114. Yu L., York J., von Bergmann K., Lutjohann D., Cohen J.C., and Hobbs H.H. J. Biol. Chem. 278 (2003) 15565
115. Mak P.A., Laffitte B.A., Desrumaux C., Joseph S.B., Curtiss L.K., Mangelsdorf D.J., Tontonoz P., and Edwards P.A. J. Biol. Chem. 277 (2002) 31900
116. Laffitte B.A., Repa J.J., Joseph S.B., Wilpitz D.C., Kast H.R., Mangelsdorf D.J., and Tontonoz P. Proc. Natl. Acad. Sci. USA 98 (2001) 507
117. Goldberg I.J. J. Lipid Res. 37 (1996) 693
118. Bruemmer D., and Law R.E. Curr. Drug Targets Cardiovasc. Haematol. Disord. 5 (2005) 533
119. Jaye M. Curr. Opin. Investig. Drugs 4 (2003) 1053
120. Lund E.G., Menke J.G., and Sparrow C.P. Arterioscler. Thromb. Vasc. Biol. 23 (2003) 1169
121. Schuster G.U., Parini P., Wang L., Alberti S., Steffensen K.R., Hansson G.K., Angelin B., and Gustafsson J.A. Circulation 106 (2002) 1147
122. Joseph S.B., McKilligin E., Pei L., Watson M.A., Collins A.R., A Laffitte B., Chen M., Noh G., Goodman J., Hagger G.N., Tran J., Tippin T.K., Wang X., Lusis A.J., Hsueh W.A., Law R.E., Collins J.L., Willson T.M., and Tontonoz P. Proc. Natl. Acad. Sci. USA 99 (2002) 7604
123. Schultz J.R., Tu H., Luk A., Repa J.J., Medina J.C., Li L., Schwendner S., Wang S., Thoolen M., Mangelsdorf D.J., Lustig K.D., and Shan B. Genes Dev. 14 (2000) 2831
124. Repa J.J., Liang G., Ou J., Bashmakov Y., Lobaccaro J.M., Shimomura I., Shan B., Brown M.S., Goldstein J.L., and Mangelsdorf D.J. Genes Dev. 14 (2000) 2819
125. Peet D.J., Turley S.D., Ma W., Janowski B.A., Lobaccaro J., Hammer R.E., and Mangelsdorf D.J. Cell 93 (1998) 693
126. Lund E.G., Peterson L.B., Adams A.D., Lam M.H., Burton C.A., Chin J., Guo Q., Huang S., Latham M., Lopez J.C., Menke J.G., Milot D.P., Mitnaul L.J., Rex-Rabe S.E., Rosa R.L., Tian J.Y., Wright S.D., and Sparrow C.P. Biochem. Pharmacol. 71 (2006) 453
127. Song C., and Liao S. Steroids 66 (2001) 673
128. Horton J.D., Goldstein J.L., and Brown M.S. J. Clin. Invest. 109 (2002) 1125
129. Michael L.F., Schkeryantz J.M., and Burris T.P. Mini Rev. Med. Chem. 5 (2005) 729
130. Lala D.S. Curr. Opin. Investig. Drugs 6 (2005) 934
131. Cao G., Liang Y., Jiang X.C., and Eacho P.I. Drug News Perspect. 17 (2004) 35
132. Gong H., and Xie W. Expert Opin. Ther. Targets 8 (2004) 49
133. Wang L., Schuster G.U., Hultenby K., Zhang Q., Andersson S., and Gustafsson J.A. Proc. Natl. Acad. Sci. USA. 99 (2002) 13878
134. Whitney K.D., Watson M.A., Collins J.L., Benson W.G., Stone T.M., Numerick M.J., Tippin T.K., Wilson J.G., Winegar D.A., and Kliewer S.A. Mol. Endocrinol. 16 (2002) 1378
135. Koldamova R.P., Lefterov I.M., Ikonomovic M.D., Skoko J., Lefterov P.I., Isanski B.A., DeKosky S.T., and Lazo. J.S. J. Biol. Chem. 278 (2003) 13244
136. Collins J.L. Curr. Opin. Drug Discov. Devel. 7 (2004) 692
137. Koldamova R.D. J. Biol. Chem. 278 (2003) 13244
138. Sun Y., Yao J., Kim T.W., and Tall A.R. J. Biol. Chem. 278 (2003) 27688
139. Fukumoto H., Deng A., Irizarry M.C., Fitzgerald M.L., and Rebeck G.W. J. Biol. Chem. 277 (2002) 48508
140. Recent LXR Medicinal Chemistry Reviews: (a). L. Michael, Mini Rev. Med. Chem. 2005, 5, 729. (b) J. Collins, Curr. Opin. Drug Discov. Devel. 2004, 7, 692.
141. Jaye M.C., Krawiec J.A., Campobasso N., Smallwood A., Qiu C., Lu Q., Kerrigan J.J., De Los Frailes Alvaro M., Laffitte B., Liu W.S., Marino Jr J.P., Meyer C.R., Nichols J.A., Parks D.J., Perez P., Sarov-Blat L., Seepersaud S.D., Steplewski K.M., Thompson S.K., Wang P., Watson M.A., Webb C.L., Haigh D., Caravella J.A., Macphee C.H., Willson T.M., and Collins J.L. J. Med. Chem. 48 (2005) 5419
142. C. Boström, J. Brickmann, K. Holm, P. Sandberg, P. Swanson and M. Westerlund, WO Patent 005417 A1, 2005.
143. P. Holm, WO Patent 005416 A1, 2005.
144. Szewczyk J.W., Huang S., Chin J., Tian J., Mitnaul L., Rosa R.L., Peterson L., Sparrow C.P., and Adams A.D. Bioorg. Med. Chem. Lett. 16 (2006) 3055
145. Singh S.B., Ondeyka J.G., Liu W., Chen S., Chen T.S., Li X., Bouffard A., Dropinski J., Jones A.B., McCormick S., Hayes N., Wang J., Sharma N., Macnaul K., Hernandez M., Chao Y.S., Baffic J., Lam M.H., Burton C., Sparrow C.P., and Menke J.G. Bioorg. Med. Chem. Lett. 15 (2005) 2824
146. Liu W., Chen S., Dropinski J., Colwell L., Robins M., Szymonifka M., Hayes N., Sharma N., MacNaul K., Hernandez M., Burton C., Sparrow C.P., Menke J.G., and Singh S.B. Bioorg. Med. Chem. Lett. 15 (2005) 4574
147. Jayasuriya H., Herath K.B., Ondeyka J.G., Guan Z., Borris R.P., Tiwari S., de Jong W., Chavez F., Moss D. W. Stevenson J., Beck H.T., Slattery M., Zamora N., Schulman M., Ali A., Sharma N., MacNaul K., Hayes N., Menke J.G., and Singh S.B. J. Nat. Prod. 68 (2005) 1247
148. Tamehiro N., Sato Y., Suzuki T., Hashimoto T., Asakawa Y., Yokoyama S., Kawanishi T., Ohno Y., Inoue K., Nagao T., and Nishimaki-Mogami T. FEBS Lett. 579 (2005) 5299
149. Huang T.H., Razmovski-Naumovski V., Salam N.K., Duke R.K., Tran V.H., Duke C.C., and Roufogalis B.D. Biochem. Pharmacol. 70 (2005) 1298
150. Surugiu-Warnmark I., Warnmark A., Toresson G., Gustafsson J.A., and Bulow L. Biochem. Biophys. Res. Commun. 332 (2005) 512
151. S. Huang and A. D. Adams, US Patent 0113419 A1, 2005.
152. I. Deuschle, U. Kögl, M. Blume, B. Albers and M. Kober, WO Patent 04024161A1, 2004.
153. S. Golz, U. Bruggemeier and A. Geerts, WO Patent 101011 A2, 2005.
154. T. H. Hoang, S. K. Thompson and D. G. Washburn, WO Patent 05023196A2, 2005.
155. T. H. Hoang, S. K. Thompson and D. G. Washburn, WO Patent 05023247A1, 2005.
156. L. S. Kallander, J. P. Marino and S. K.. Thompson, WO Patent 05023188A2, 2005.
157. H. Kikkawa, M. Kinoshita and O. Kurusu, WO Patent 05055998A1, 2005. (b) S. B. Joseph, A. Castrillo, B. A. Laffitte, D. J. Mangelsdorf and P. Tontonoz., Nat. Med., 2003, 9, 213.
158. H. Dehmlow, R. Masciadri, N. Panday, H. Ratni and M. B. Wright, US Patent 0004068A1, 2006.
159. H. Dehmlow, N. Panday, H. Ratni, T. Schulz-Gasch and M. B. Wright, US Patent 0245515, 2005.
160. M. Arai, S. Kaneko, S. Shibuya, T. Watanabe and Y. Kumakura, WO Patent 023782 A1, 2005.
161. R. J. Steffan,. E. M. Matelan, S. M. Bowen, J. W. Ullrich, J. E. Wrobel, E. Zamaratski, L. Kruger, A. L. Olsen, A. Cheng, T. Hansson, R. J. Uunwalla, C. P. Miller, P. P. Rhönnstad, WO Patent 017384A2, 2006.
162. M. D. Collini, R. R.Singhaus, B. Hu, J. W. Jetter, R. L. Morris, D. H. Kaufman, C. P. Miller, J. W. Ullrich, R. J. Unwalla, J. E. Wrobel, E. Quinet, P. Nambi, R. C. Bernotas, M. Elloso, WO Patent 058834A2, 2005.
163. C. D. Bayne, A. T. Johnson, S. Lu, R. Mohan, M. C. Nyman, E. J. Schweiger, W. C. Stevens, H. Wang and Y. Xie, US Patent 0080111 A1, 2005.
164. V. Molteni, X. Li, J. Nanakka, D. A. Ellis, B. Anaclerio, E. Saez and J. Wityak, WO Patent 077124, 2005.
165. P. Diaz, J. Bernardon and E. Thoreau, WO Patent 076418A1, 2004.
166. L. Li, J. C. Medina and B. Shan, US Patent 6906069 B1, 2005.
167. Pellicciari R., Gioiello A., and Costantino G. Expert Opin. Ther. Patents 16 (2006) 333
168. Westin S., Heyman R.A., and Martin R. Mini Rev. Med. Chem. 5 (2005) 719
169. Pellicciari R., Costantino G., and Fiorucci S. J. Med. Chem. 48 (2005) 5383
170. Repa J.J., Turley S.D., Lobaccaro J.A., Medina J., Li L., Lustig K., Shan B., Heyman R.A., Dietschy J.M., and Mangelsdorf D.J. Science 289 (2000) 1524
171. Yang Y., Zhang M., Eggertsen G., and Chiang J.Y. Biochim. Biophys. Acta. 1583 (2002) 63
172. Sinal C.J., Tohkin M., Miyata M., Ward J.M., Lambert G., and Gonzalez F.J. Cell 102 (2000) 731
173. Nicolaou K.C., Evans R.M., Roecker A.J., Hughes R., Downes M., and Pfefferkorn J.A. Org. Biomol. Chem. 1 (2003) 908
174. Honorio K.M., Garratt R.C., and Andricopulo A.D. Bioorg. Med. Chem. Lett. 15 (2005) 3119
175. Maloney P.R., Parks D.J., Haffner C.D., Fivush A.M., Chandra G., Plunket K.D., Creech K.L., Moore L.B., Wilson J.G., Lewis M.C., Jones S.A., and M Willson T. J. Med. Chem. 43 (2000) 2971
176. Urizar N.L., Liverman A.B., Dodds D.T., Silva F.V., Ordentlich P., Yan Y., Gonzalez F.J., Heyman R.A., Mangelsdorf D.J., and Moore D.D. Science 296 (2002) 1703
177. Cui J., Huang L., Zhao A., Lew J.L., Yu J., Sahoo S., Meinke P.T., Royo I., Pelaez F., and Wright S.D. J. Biol. Chem. 278 (2003) 10214
178. Wu J., Xia C., Meier J., Li S., Hu X., and Lala D.S. Mol. Endocrinol. 16 (2002) 1590
179. Szapary P.O., Wolfe M.L., Bloedon L.T., Cucchiara A.J., DerMarderosian A.H., Cirigliano M.D., and Rader D.J. JAMA 290 (2003) 765