-
1
-
-
84907943686
-
Polypharmacology: Challenges and opportunities in drug discovery
-
Anighoro A, Bajorath J, Rastelli G (2014) Polypharmacology: challenges and opportunities in drug discovery. J Med Chem 57:7874-7887
-
(2014)
J Med Chem
, vol.57
, pp. 7874-7887
-
-
Anighoro, A.1
Bajorath, J.2
Rastelli, G.3
-
2
-
-
84991295067
-
-
Banyu Pharmaceutical, Tokyo. WO2010104195A1
-
Arakawa K, Nishimura T, Sugimoto Y, Takahashi H, Shimamura T (2010) Preparation of heteroaryloxyphenyldihydrobenzisothiazoledioxide derivatives and analogs for use as GPR120 receptor modulators. Banyu Pharmaceutical, Tokyo. WO2010104195A1
-
(2010)
Preparation of Heteroaryloxyphenyldihydrobenzisothiazoledioxide Derivatives and Analogs for Use as GPR120 Receptor Modulators
-
-
Arakawa, K.1
Nishimura, T.2
Sugimoto, Y.3
Takahashi, H.4
Shimamura, T.5
-
3
-
-
84937416706
-
The promise and peril of chemical probes
-
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J et al (2015) The promise and peril of chemical probes. Nat Chem Biol 11:536-541
-
(2015)
Nat Chem Biol
, vol.11
, pp. 536-541
-
-
Arrowsmith, C.H.1
Audia, J.E.2
Austin, C.3
Baell, J.4
Bennett, J.5
Blagg, J.6
-
4
-
-
84991380589
-
A non-acidic free fatty acid receptor 4 agonists with antidiabetic activity
-
Azevedo CM, Watterson KR, Wargent ET, Hansen SVF, Hudson BD, Kepczynska M et al (2016) A non-acidic free fatty acid receptor 4 agonists with antidiabetic activity. J Med Chem 59:8868-8878. doi:10.1021/acs.jmedchem.6b00685
-
(2016)
J Med Chem
, vol.59
, pp. 8868-8878
-
-
Azevedo, C.M.1
Watterson, K.R.2
Wargent, E.T.3
Hansen, S.4
Hudson, B.D.5
Kepczynska, M.6
-
5
-
-
77950571108
-
New substructure filters for removal of Pan Assay Interference Compounds (PAINS) from screening libraries and for their exclusion in bioassays
-
Baell JB, Holloway GA (2010) New substructure filters for removal of Pan Assay Interference Compounds (PAINS) from screening libraries and for their exclusion in bioassays. J Med Chem 53:2719-2740
-
(2010)
J Med
, vol.53
, pp. 2719-2740
-
-
Baell, J.B.1
Holloway, G.A.2
-
6
-
-
79955856369
-
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): A novel multimodal compound for the treatment of major depressive disorder
-
Bang-Andersen B, Ruhland T, Jorgensen M, Smith G, Frederiksen K, Jensen KG et al (2011) Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem 54:3206-3221
-
(2011)
J Med Chem
, vol.54
, pp. 3206-3221
-
-
Bang-Andersen, B.1
Ruhland, T.2
Jorgensen, M.3
Smith, G.4
Frederiksen, K.5
Jensen, K.G.6
-
7
-
-
84929687810
-
Choosing the right tool for the job: RNAi, TALEN, or CRISPR
-
Boettcher M, McManus MT (2015) Choosing the right tool for the job: RNAi, TALEN, or CRISPR. Mol Cell 58:575-585
-
(2015)
Mol Cell
, vol.58
, pp. 575-585
-
-
Boettcher, M.1
McManus, M.T.2
-
8
-
-
33745607930
-
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: Identification of agonist and antagonist small molecules
-
Briscoe CP, Peat AJ, McKeown SC, Corbett DF, Goetz AS, Littleton TR et al (2006) Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol 148:619-628
-
(2006)
Br J Pharmacol
, vol.148
, pp. 619-628
-
-
Briscoe, C.P.1
Peat, A.J.2
McKeown, S.C.3
Corbett, D.F.4
Goetz, A.S.5
Littleton, T.R.6
-
10
-
-
84903513580
-
Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4
-
Butcher AJ, Hudson BD, Shimpukade B, Alvarez-Curto E, Prihandoko R, Ulven T et al (2014) Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4. J Biol Chem 289:18451-18465
-
(2014)
J Biol Chem
, vol.289
, pp. 18451-18465
-
-
Butcher, A.J.1
Hudson, B.D.2
Shimpukade, B.3
Alvarez-Curto, E.4
Prihandoko, R.5
Ulven, T.6
-
11
-
-
84858243360
-
Mechanisms of action of (N-3) fatty acids
-
Calder PC (2012) Mechanisms of action of (n-3) fatty acids. J Nutr 142:592s-599s
-
(2012)
J Nutr
, vol.142
, pp. 592s-599s
-
-
Calder, P.C.1
-
12
-
-
85037119892
-
-
Merck Sharp & Dohme, Kenilworth, NJ. WO2014059232A2
-
Chelliah M, Chu HD, Cox JM, Debenham JS, Eagen K, Lan P et al (2014) Preparation of substituted spiropiperidinyl compounds useful as GPR120 agonists. Merck Sharp & Dohme, Kenilworth, NJ. WO2014059232A2
-
(2014)
Preparation of Substituted Spiropiperidinyl Compounds Useful as GPR120 Agonists
-
-
Chelliah, M.1
Chu, H.D.2
Cox, J.M.3
Debenham, J.S.4
Eagen, K.5
Lan, P.6
-
13
-
-
80053910894
-
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties
-
Christiansen E, Urban C, Grundmann M, Due-Hansen ME, Hagesaether E, Schmidt J et al (2011) Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. J Med Chem 54:6691-6703
-
(2011)
J Med Chem
, vol.54
, pp. 6691-6703
-
-
Christiansen, E.1
Urban, C.2
Grundmann, M.3
Due-Hansen, M.E.4
Hagesaether, E.5
Schmidt, J.6
-
14
-
-
84864228135
-
Free fatty acid receptor 1 (FFA1/GPR40) agonists: Mesylpropoxy appendage lowers lipophilicity and improves ADME properties
-
Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schroder R, Hudson BD et al (2012) Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J Med Chem 55:6624-6628
-
(2012)
J Med Chem
, vol.55
, pp. 6624-6628
-
-
Christiansen, E.1
Due-Hansen, M.E.2
Urban, C.3
Grundmann, M.4
Schroder, R.5
Hudson, B.D.6
-
15
-
-
84873900885
-
Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability
-
Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schmidt J, Hansen SVF et al (2013) Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. J Med Chem 56:982-992
-
(2013)
J Med Chem
, vol.56
, pp. 982-992
-
-
Christiansen, E.1
Due-Hansen, M.E.2
Urban, C.3
Grundmann, M.4
Schmidt, J.5
Hansen, S.6
-
16
-
-
84930924216
-
Activity of dietary fatty acids on FFA1 and FFA4 and characterization of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases
-
Christiansen E, Watterson KR, Stocker CJ, Sokol E, Jenkins L, Simon K et al (2015) Activity of dietary fatty acids on FFA1 and FFA4 and characterization of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases. Br J Nutr 113:1677-1688
-
(2015)
Br J Nutr
, vol.113
, pp. 1677-1688
-
-
Christiansen, E.1
Watterson, K.R.2
Stocker, C.J.3
Sokol, E.4
Jenkins, L.5
Simon, K.6
-
17
-
-
84855971481
-
Unsaturated fatty acids revert diet-induced hypothalamic inflammation in obesity
-
Cintra DE, Ropelle ER, Moraes JC, Pauli JR, Morari J, Souza CT et al (2012) Unsaturated fatty acids revert diet-induced hypothalamic inflammation in obesity. PLoS One 7, e30571
-
(2012)
Plos One
, vol.7
-
-
Cintra, D.E.1
Ropelle, E.R.2
Moraes, J.C.3
Pauli, J.R.4
Morari, J.5
Souza, C.T.6
-
18
-
-
54349086815
-
Modulation of osteoclastogenesis by fatty acids
-
Cornish J, MacGibbon A, Lin JM, Watson M, Callon KE, Tong PC et al (2008) Modulation of osteoclastogenesis by fatty acids. Endocrinology 149:5688-5695
-
(2008)
Endocrinology
, vol.149
, pp. 5688-5695
-
-
Cornish, J.1
Macgibbon, A.2
Lin, J.M.3
Watson, M.4
Callon, K.E.5
Tong, P.C.6
-
19
-
-
84878371294
-
International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands
-
Davenport AP, Alexander SPH, Sharman JL, Pawson AJ, Benson HE, Monaghan AE et al (2013) International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev 65:967-986
-
(2013)
Pharmacol Rev
, vol.65
, pp. 967-986
-
-
Davenport, A.P.1
Alexander, S.2
Sharman, J.L.3
Pawson, A.J.4
Benson, H.E.5
Monaghan, A.E.6
-
20
-
-
84902546389
-
Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus
-
Defossa E, Wagner M (2014) Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus. Bioorg Med Chem Lett 24:2991-3000
-
(2014)
Bioorg Med Chem Lett
, vol.24
, pp. 2991-3000
-
-
Defossa, E.1
Wagner, M.2
-
21
-
-
79151478555
-
Type 2 diabetes as an inflammatory disease
-
Donath MY, Shoelson SE (2011) Type 2 diabetes as an inflammatory disease. Nat Rev Immunol 11:98-107
-
(2011)
Nat Rev Immunol
, vol.11
, pp. 98-107
-
-
Donath, M.Y.1
Shoelson, S.E.2
-
22
-
-
84946061687
-
Transcriptional and functional characterization of the G protein-coupled receptor repertoire of gastric somatostatin cells
-
Egerod KL, Engelstoft MS, Lund ML, Grunddal KV, Zhao M, Barir-Jensen D et al (2015) Transcriptional and functional characterization of the G protein-coupled receptor repertoire of gastric somatostatin cells. Endocrinology 156:3909-3923
-
(2015)
Endocrinology
, vol.156
, pp. 3909-3923
-
-
Egerod, K.L.1
Engelstoft, M.S.2
Lund, M.L.3
Grunddal, K.V.4
Zhao, M.5
Barir-Jensen, D.6
-
23
-
-
84889093491
-
Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells
-
Engelstoft MS, Park WM, Sakata I, Kristensen LV, Husted AS, Osborne-Lawrence S et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2:376-392
-
(2013)
Mol Metab
, vol.2
, pp. 376-392
-
-
Engelstoft, M.S.1
Park, W.M.2
Sakata, I.3
Kristensen, L.V.4
Husted, A.S.5
Osborne-Lawrence, S.6
-
24
-
-
85050577926
-
FFA4/GPR120 agonists: A survey of the recent patent literature
-
Formicola R, Pevarello P, Kuhn C, Liberati C, Piscitelli F, Sodano M (2015) FFA4/GPR120 agonists: a survey of the recent patent literature. Pharm Pat Anal 4:443-451
-
(2015)
Pharm Pat Anal
, vol.4
, pp. 443-451
-
-
Formicola, R.1
Pevarello, P.2
Kuhn, C.3
Liberati, C.4
Piscitelli, F.5
Sodano, M.6
-
25
-
-
77249142404
-
The art of the chemical probe
-
Frye SV (2010) The art of the chemical probe. Nat Chem Biol 6:159-161
-
(2010)
Nat Chem Biol
, vol.6
, pp. 159-161
-
-
Frye, S.V.1
-
26
-
-
84940955742
-
Different roles of GPR120 and GPR40 in the acquisition of malignant properties in pancreatic cancer cells
-
Fukushima K, Yamasaki E, Ishii S, Tomimatsu A, Takahashi K, Hirane M et al (2015) Different roles of GPR120 and GPR40 in the acquisition of malignant properties in pancreatic cancer cells. Biochem Biophys Res Commun 465:512-515
-
(2015)
Biochem Biophys Res Commun
, vol.465
, pp. 512-515
-
-
Fukushima, K.1
Yamasaki, E.2
Ishii, S.3
Tomimatsu, A.4
Takahashi, K.5
Hirane, M.6
-
27
-
-
84941702458
-
GPR120: A bi-potential mediator to modulate the osteogenic and adipogenic differentiation of BMMSCs
-
Gao B, Huang Q, Jie Q, Lu W-G, Wang L, Li X-J et al (2015) GPR120: a bi-potential mediator to modulate the osteogenic and adipogenic differentiation of BMMSCs. Sci Rep 5:14080
-
(2015)
Sci Rep
, vol.5
, pp. 14080
-
-
Gao, B.1
Huang, Q.2
Jie, Q.3
Lu, W.-G.4
Wang, L.5
Li, X.-J.6
-
28
-
-
80053155457
-
Unsaturated fatty acids stimulate LH secretion via novel PKCepsilon and -theta in gonadotrope cells and inhibit GnRH-induced LH release
-
Garrel G, Simon V, Denoyelle C, Cruciani-Guglielmacci C, Migrenne S, Counis R et al (2011) Unsaturated fatty acids stimulate LH secretion via novel PKCepsilon and -theta in gonadotrope cells and inhibit GnRH-induced LH release. Endocrinology 152:3905-3916
-
(2011)
Endocrinology
, vol.152
, pp. 3905-3916
-
-
Garrel, G.1
Simon, V.2
Denoyelle, C.3
Cruciani-Guglielmacci, C.4
Migrenne, S.5
Counis, R.6
-
29
-
-
84891553727
-
G protein-coupled receptor 120 signaling regulates ghrelin secretion in vivo and in vitro
-
Gong Z, Yoshimura M, Aizawa S, Kurotani R, Zigman JM, Sakai T et al (2014) G protein-coupled receptor 120 signaling regulates ghrelin secretion in vivo and in vitro. Am J Physiol Endocrinol Metab 306:E28-E35
-
(2014)
Am J Physiol Endocrinol Metab
, vol.306
, pp. E28-E35
-
-
Gong, Z.1
Yoshimura, M.2
Aizawa, S.3
Kurotani, R.4
Zigman, J.M.5
Sakai, T.6
-
30
-
-
84973162103
-
Treatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice
-
Gozal D, Qiao Z, Almendros I, Zheng J, Khalyfa A, Shimpukade B et al (2016) Treatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice. Int J Obes 40:1143-1149
-
(2016)
Int J Obes
, vol.40
, pp. 1143-1149
-
-
Gozal, D.1
Qiao, Z.2
Almendros, I.3
Zheng, J.4
Khalyfa, A.5
Shimpukade, B.6
-
31
-
-
84946499740
-
Obesity and altered sleep: A pathway to metabolic derangements in children?
-
Hakim F, Kheirandish-Gozal L, Gozal D (2015a) Obesity and altered sleep: a pathway to metabolic derangements in children? Semin Pediatr Neurol 22:77-85
-
(2015)
Semin Pediatr Neurol
, vol.22
, pp. 77-85
-
-
Hakim, F.1
Kheirandish-Gozal, L.2
Gozal, D.3
-
32
-
-
84920385377
-
Chronic sleep fragmentation during the sleep period induces hypothalamic endoplasmic reticulum stress and PTP1b-mediated leptin resistance in male mice
-
Hakim F, Wang Y, Carreras A, Hirotsu C, Zhang J, Peris E et al (2015b) Chronic sleep fragmentation during the sleep period induces hypothalamic endoplasmic reticulum stress and PTP1b-mediated leptin resistance in male mice. Sleep 38:31-40
-
(2015)
Sleep
, vol.38
, pp. 31-40
-
-
Hakim, F.1
Wang, Y.2
Carreras, A.3
Hirotsu, C.4
Zhang, J.5
Peris, E.6
-
33
-
-
84890063785
-
The therapeutic potential of GPR120: A patent review
-
Halder S, Kumar S, Sharma R (2013) The therapeutic potential of GPR120: a patent review. Expert Opin Ther Pat 23:1581-1590
-
(2013)
Expert Opin Ther Pat
, vol.23
, pp. 1581-1590
-
-
Halder, S.1
Kumar, S.2
Sharma, R.3
-
34
-
-
13444263540
-
Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
-
Hirasawa A, Tsumaya K, Awaji T, Katsuma S, Adachi T, Yamada M et al (2005) Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120. Nat Med 11:90-94
-
(2005)
Nat Med
, vol.11
, pp. 90-94
-
-
Hirasawa, A.1
Tsumaya, K.2
Awaji, T.3
Katsuma, S.4
Adachi, T.5
Yamada, M.6
-
35
-
-
33745148616
-
Very-long-chain and branched-chain fatty acyl-CoAs are high affinity ligands for the peroxisome proliferator-activated receptor α (PPARα)
-
Hostetler HA, Kier AB, Schroeder F (2006) Very-long-chain and branched-chain fatty acyl-CoAs are high affinity ligands for the peroxisome proliferator-activated receptor α (PPARα). Biochemistry 45:7669-7681
-
(2006)
Biochemistry
, vol.45
, pp. 7669-7681
-
-
Hostetler, H.A.1
Kier, A.B.2
Schroeder, F.3
-
36
-
-
84880787550
-
Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids
-
Hudson BD, Murdoch H, Milligan G (2013a) Minireview: the effects of species ortholog and SNP variation on receptors for free fatty acids. Mol Endocrinol 27:1177-1187
-
(2013)
Mol Endocrinol
, vol.27
, pp. 1177-1187
-
-
Hudson, B.D.1
Murdoch, H.2
Milligan, G.3
-
37
-
-
84886060164
-
The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism
-
Hudson BD, Shimpukade B, Mackenzie AE, Butcher AJ, Pediani JD, Christiansen E et al (2013b) The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism. Mol Pharmacol 84:710-725
-
(2013)
Mol Pharmacol
, vol.84
, pp. 710-725
-
-
Hudson, B.D.1
Shimpukade, B.2
Mackenzie, A.E.3
Butcher, A.J.4
Pediani, J.D.5
Christiansen, E.6
-
38
-
-
84904512037
-
The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120)
-
Hudson BD, Shimpukade B, Milligan G, Ulven T (2014) The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120). J Biol Chem 289:20345-20358
-
(2014)
J Biol Chem
, vol.289
, pp. 20345-20358
-
-
Hudson, B.D.1
Shimpukade, B.2
Milligan, G.3
Ulven, T.4
-
39
-
-
64249111493
-
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists
-
Humphries PS, Benbow JW, Bonin PD, Boyer D, Doran SD, Frisbie RK et al (2009) Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists. Bioorg Med Chem Lett 19:2400-2403
-
(2009)
Bioorg Med Chem Lett
, vol.19
, pp. 2400-2403
-
-
Humphries, P.S.1
Benbow, J.W.2
Bonin, P.D.3
Boyer, D.4
Doran, S.D.5
Frisbie, R.K.6
-
40
-
-
84919624949
-
Opposite effects of GPR120 and GPR40 on cell motile activity induced by ethionine in liver epithelial cells
-
Ishii S, Hirane M, Kato S, Fukushima N, Tsujiuchi T (2015a) Opposite effects of GPR120 and GPR40 on cell motile activity induced by ethionine in liver epithelial cells. Biochem Biophys Res Commun 456:135-138
-
(2015)
Biochem Biophys Res Commun
, vol.456
, pp. 135-138
-
-
Ishii, S.1
Hirane, M.2
Kato, S.3
Fukushima, N.4
Tsujiuchi, T.5
-
41
-
-
84922073819
-
Role of GPR120 in cell motile activity induced by 12-O-tetradecanoylphorbol-13-acetate in liver epithelial WB-F344 cells
-
Ishii S, Hirane M, Kitamura Y, Mori S, Fukushima N, Honoki K et al (2015b) Role of GPR120 in cell motile activity induced by 12-O-tetradecanoylphorbol-13-acetate in liver epithelial WB-F344 cells. Mol Cell Biochem 400:145-151
-
(2015)
Mol Cell Biochem
, vol.400
, pp. 145-151
-
-
Ishii, S.1
Hirane, M.2
Kitamura, Y.3
Mori, S.4
Fukushima, N.5
Honoki, K.6
-
42
-
-
84940773131
-
G protein-coupled receptor 120 signaling negatively regulates osteoclast differentiation, survival, and function
-
Kim HJ, Yoon HJ, Kim BK, Kang WY, Seong SJ, Lim MS et al (2015) G protein-coupled receptor 120 signaling negatively regulates osteoclast differentiation, survival, and function. J Cell Physiol 231:844-851
-
(2015)
J Cell Physiol
, vol.231
, pp. 844-851
-
-
Kim, H.J.1
Yoon, H.J.2
Kim, B.K.3
Kang, W.Y.4
Seong, S.J.5
Lim, M.S.6
-
43
-
-
84960156185
-
Diverse effects of G-protein-coupled free fatty acid receptors on the regulation of cellular functions in lung cancer cells
-
Kita T, Kadochi Y, Takahashi K, Fukushima K, Yamasaki E, Uemoto T et al (2016) Diverse effects of G-protein-coupled free fatty acid receptors on the regulation of cellular functions in lung cancer cells. Exp Cell Res 342:193-199
-
(2016)
Exp Cell Res
, vol.342
, pp. 193-199
-
-
Kita, T.1
Kadochi, Y.2
Takahashi, K.3
Fukushima, K.4
Yamasaki, E.5
Uemoto, T.6
-
44
-
-
77249176182
-
Rethinking screening
-
Kodadek T (2010) Rethinking screening. Nat Chem Biol 6:162-165
-
(2010)
Nat Chem Biol
, vol.6
, pp. 162-165
-
-
Kodadek, T.1
-
45
-
-
84925651447
-
Functional analysis of free fatty acid receptor GPR120 in human eosinophils: Implications in metabolic homeostasis
-
Konno Y, Ueki S, Takeda M, Kobayashi Y, Tamaki M, Moritoki Y et al (2015) Functional analysis of free fatty acid receptor GPR120 in human eosinophils: implications in metabolic homeostasis. PLoS One 10, e0120386
-
(2015)
Plos One
, vol.10
-
-
Konno, Y.1
Ueki, S.2
Takeda, M.3
Kobayashi, Y.4
Tamaki, M.5
Moritoki, Y.6
-
46
-
-
84886511483
-
FFAR1 is involved in both the acute and chronic effects of palmitate on insulin secretion
-
Kristinsson H, Smith DM, Bergsten P, Sargsyan E (2013) FFAR1 is involved in both the acute and chronic effects of palmitate on insulin secretion. Endocrinology 154:4078-4088
-
(2013)
Endocrinology
, vol.154
, pp. 4078-4088
-
-
Kristinsson, H.1
Smith, D.M.2
Bergsten, P.3
Sargsyan, E.4
-
47
-
-
4043140077
-
Polyunsaturated fatty acids including docosahexaenoic and arachidonic acid bind to the retinoid X receptor alpha ligand-binding domain
-
Lengqvist J, Mata De Urquiza A, Bergman AC, Willson TM, Sjovall J, Perlmann T et al (2004) Polyunsaturated fatty acids including docosahexaenoic and arachidonic acid bind to the retinoid X receptor alpha ligand-binding domain. Mol Cell Proteomics 3:692-703
-
(2004)
Mol Cell Proteomics
, vol.3
, pp. 692-703
-
-
Lengqvist, J.1
Mata De Urquiza, A.2
Bergman, A.C.3
Willson, T.M.4
Sjovall, J.5
Perlmann, T.6
-
48
-
-
84886264421
-
Cyclooxygenase-2 induction in macrophages is modulated by docosahexaenoic acid via interactions with free fatty acid receptor 4 (FFA4)
-
Li X, Yu Y, Funk CD (2013a) Cyclooxygenase-2 induction in macrophages is modulated by docosahexaenoic acid via interactions with free fatty acid receptor 4 (FFA4). FASEB J 27:4987-4997
-
(2013)
FASEB J
, vol.27
, pp. 4987-4997
-
-
Li, X.1
Yu, Y.2
Funk, C.D.3
-
49
-
-
84876012123
-
Hyperhomocysteinemia promotes insulin resistance by inducing endoplasmic reticulum stress in adipose tissue
-
Li Y, Zhang H, Jiang C, Xu M, Pang Y, Feng J et al (2013b) Hyperhomocysteinemia promotes insulin resistance by inducing endoplasmic reticulum stress in adipose tissue. J Biol Chem 288:9583-9592
-
(2013)
J Biol Chem
, vol.288
, pp. 9583-9592
-
-
Li, Y.1
Zhang, H.2
Jiang, C.3
Xu, M.4
Pang, Y.5
Feng, J.6
-
50
-
-
84904904848
-
The fish oil ingredient, docosahexaenoic acid, activates cytosolic phospholipase A(2) via GPR120 receptor to produce prostaglandin E(2) and plays an anti-inflammatory role in macrophages
-
Liu Y, Chen LY, Sokolowska M, Eberlein M, Alsaaty S, Martinez-Anton A et al (2014) The fish oil ingredient, docosahexaenoic acid, activates cytosolic phospholipase A(2) via GPR120 receptor to produce prostaglandin E(2) and plays an anti-inflammatory role in macrophages. Immunology 143:81-95
-
(2014)
Immunology
, vol.143
, pp. 81-95
-
-
Liu, Y.1
Chen, L.Y.2
Sokolowska, M.3
Eberlein, M.4
Alsaaty, S.5
Martinez-Anton, A.6
-
51
-
-
84921316458
-
Omega-3 fatty acids and other FFA4 agonists inhibit growth factor signaling in human prostate cancer cells
-
Liu Z, Hopkins MM, Zhang Z, Quisenberry CB, Fix LC, Galvan BM et al (2015) Omega-3 fatty acids and other FFA4 agonists inhibit growth factor signaling in human prostate cancer cells. J Pharmacol Exp Ther 352:380-394
-
(2015)
J Pharmacol Exp Ther
, vol.352
, pp. 380-394
-
-
Liu, Z.1
Hopkins, M.M.2
Zhang, Z.3
Quisenberry, C.B.4
Fix, L.C.5
Galvan, B.M.6
-
52
-
-
85014118861
-
-
Metabolex, Hayward, CA. WO2010048207A2
-
Ma J, Novack A, Nashashibi I, Pham P, Rabbat CJ, Song J et al (2010) [(Heterocyclylmethoxy) aryl]alkanoic acid derivatives as GPR120 receptor agonists and preparation and uses thereof. Metabolex, Hayward, CA. WO2010048207A2
-
(2010)
[(Heterocyclylmethoxy) Aryl]Alkanoic Acid Derivatives as GPR120 Receptor Agonists and Preparation and Uses Thereof
-
-
Ma, J.1
Novack, A.2
Nashashibi, I.3
Pham, P.4
Rabbat, C.J.5
Song, J.6
-
53
-
-
84867347584
-
Lipid- mediated release of GLP-1 by mouse taste buds from circumvallate papillae: Putative involvement of GPR120 and impact on taste sensitivity
-
Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ et al (2012) Lipid- mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res 53:2256-2265
-
(2012)
J Lipid Res
, vol.53
, pp. 2256-2265
-
-
Martin, C.1
Passilly-Degrace, P.2
Chevrot, M.3
Ancel, D.4
Sparks, S.M.5
Drucker, D.J.6
-
54
-
-
84937398931
-
Characterising pharmacological ligands to study the long chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4
-
Milligan G, Alvarez-Curto E, Watterson KR, Ulven T, Hudson BD (2015) Characterising pharmacological ligands to study the long chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. Br J Pharmacol 172:3254-3265
-
(2015)
Br J Pharmacol
, vol.172
, pp. 3254-3265
-
-
Milligan, G.1
Alvarez-Curto, E.2
Watterson, K.R.3
Ulven, T.4
Hudson, B.D.5
-
56
-
-
84946416932
-
Novel identification of the free fatty acid receptor FFAR1 that promotes contraction in airway smooth muscle
-
Mizuta K, Zhang Y, Mizuta F, Hoshijima H, Shiga T, Masaki E et al (2015) Novel identification of the free fatty acid receptor FFAR1 that promotes contraction in airway smooth muscle. Am J Physiol Lung Cell Mol Physiol 309:L970-L982
-
(2015)
Am J Physiol Lung Cell Mol Physiol
, vol.309
, pp. L970-L982
-
-
Mizuta, K.1
Zhang, Y.2
Mizuta, F.3
Hoshijima, H.4
Shiga, T.5
Masaki, E.6
-
57
-
-
84956620224
-
Free-fatty acid receptor-4 (GPR120): Cellular and molecular function and its role in metabolic disorders
-
Moniri NH (2016) Free-fatty acid receptor-4 (GPR120): cellular and molecular function and its role in metabolic disorders. Biochem Pharmacol 110-111:1-15
-
(2016)
Biochem Pharmacol
, vol.110-111
, pp. 1-15
-
-
Moniri, N.H.1
-
58
-
-
84891859045
-
Free fatty acid (FFA) and hydroxy carboxylic acid (HCA) receptors
-
Offermanns S (2014) Free fatty acid (FFA) and hydroxy carboxylic acid (HCA) receptors. Annu Rev Pharmacol Toxicol 54:407-434
-
(2014)
Annu Rev Pharmacol Toxicol
, vol.54
, pp. 407-434
-
-
Offermanns, S.1
-
59
-
-
84959340392
-
G protein-coupled receptors as targets for anti-diabetic therapeutics
-
Oh da Y, Olefsky JM (2016) G protein-coupled receptors as targets for anti-diabetic therapeutics. Nat Rev Drug Discov 15:161-172
-
(2016)
Nat Rev Drug Discov
, vol.15
, pp. 161-172
-
-
Oh Da, Y.1
Olefsky, J.M.2
-
60
-
-
84907612482
-
A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice
-
Oh da Y, Walenta E, Akiyama TE, Lagakos WS, Lackey D, Pessentheiner AR et al (2014) A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Nat Med 20:942-947
-
(2014)
Nat Med
, vol.20
, pp. 942-947
-
-
Oh Da, Y.1
Walenta, E.2
Akiyama, T.E.3
Lagakos, W.S.4
Lackey, D.5
Pessentheiner, A.R.6
-
61
-
-
77956165390
-
GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects
-
Oh DY, Talukdar S, Bae EJ, Imamura T, Morinaga H, Fan WQ et al (2010) GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects. Cell 142:687-698
-
(2010)
Cell
, vol.142
, pp. 687-698
-
-
Oh, D.Y.1
Talukdar, S.2
Bae, E.J.3
Imamura, T.4
Morinaga, H.5
Fan, W.Q.6
-
62
-
-
84889262928
-
Polypharmacology - foe or friend?
-
Peters JU (2013) Polypharmacology - foe or friend? J Med Chem 56:8955-8971
-
(2013)
J Med Chem
, vol.56
, pp. 8955-8971
-
-
Peters, J.U.1
-
63
-
-
84918563561
-
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: From hit to clinic
-
Pizzonero M, Dupont S, Babel M, Beaumont S, Bienvenu N, Blanque R et al (2014) Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem 57:10044-10057
-
(2014)
J Med Chem
, vol.57
, pp. 10044-10057
-
-
Pizzonero, M.1
Dupont, S.2
Babel, M.3
Beaumont, S.4
Bienvenu, N.5
Blanque, R.6
-
64
-
-
84956696088
-
Pan Assay Interference Compounds (PAINS) and other promiscuous compounds in antifungal research
-
Pouliot M, Jeanmart S (2016) Pan Assay Interference Compounds (PAINS) and other promiscuous compounds in antifungal research. J Med Chem 59:497-503
-
(2016)
J Med Chem
, vol.59
, pp. 497-503
-
-
Pouliot, M.1
Jeanmart, S.2
-
65
-
-
84963864551
-
Distinct phosphorylation clusters determine the signaling outcome of free fatty acid receptor 4/G protein-coupled receptor 120
-
Prihandoko R, Alvarez-Curto E, Hudson BD, Butcher AJ, Ulven T, Miller AM et al (2016) Distinct phosphorylation clusters determine the signaling outcome of free fatty acid receptor 4/G protein-coupled receptor 120. Mol Pharmacol 89:505-520
-
(2016)
Mol Pharmacol
, vol.89
, pp. 505-520
-
-
Prihandoko, R.1
Alvarez-Curto, E.2
Hudson, B.D.3
Butcher, A.J.4
Ulven, T.5
Miller, A.M.6
-
66
-
-
84894058348
-
GPR120 on Kupffer cells mediates hepatoprotective effects of omega3-fatty acids
-
Raptis DA, Limani P, Jang JH, Ungethum U, Tschuor C, Graf R et al (2014) GPR120 on Kupffer cells mediates hepatoprotective effects of omega3-fatty acids. J Hepatol 60:625-632
-
(2014)
J Hepatol
, vol.60
, pp. 625-632
-
-
Raptis, D.A.1
Limani, P.2
Jang, J.H.3
Ungethum, U.4
Tschuor, C.5
Graf, R.6
-
67
-
-
84871967576
-
Polypharmacology: Drug discovery for the future
-
Reddy AS, Zhang S (2013) Polypharmacology: drug discovery for the future. Expert Rev Clin Pharmacol 6:41-47
-
(2013)
Expert Rev Clin Pharmacol
, vol.6
, pp. 41-47
-
-
Reddy, A.S.1
Zhang, S.2
-
68
-
-
84952941040
-
Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands
-
Sergeev E, Hojgaard Hansen A, Pandey SK, Mackenzie AE, Hudson BD, Ulven T et al (2015) Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands. J Biol Chem 291:303-317
-
(2015)
J Biol Chem
, vol.291
, pp. 303-317
-
-
Sergeev, E.1
Hojgaard Hansen, A.2
Pandey, S.K.3
Mackenzie, A.E.4
Hudson, B.D.5
Ulven, T.6
-
69
-
-
84901921079
-
Pro-resolving lipid mediators are leads for resolution physiology
-
Serhan CN (2014) Pro-resolving lipid mediators are leads for resolution physiology. Nature 510:92-101
-
(2014)
Nature
, vol.510
, pp. 92-101
-
-
Serhan, C.N.1
-
70
-
-
85014096907
-
-
Metabolex, Hayward,, CA. WO2010080537A1
-
Shi DF, Song J, Ma J, Novack A, Pham P, Nashashibi I et al (2010) Preparation of benzofuranyl substituted phenylalkylcarboxylic acids as Gpr120 receptor agonists. Metabolex, Hayward, CA. WO2010080537A1
-
(2010)
Preparation of Benzofuranyl Substituted Phenylalkylcarboxylic Acids as Gpr120 Receptor Agonists
-
-
Shi, D.F.1
Song, J.2
Ma, J.3
Novack, A.4
Pham, P.5
Nashashibi, I.6
-
71
-
-
84861066914
-
Discovery of a potent and selective GPR120 agonist
-
Shimpukade B, Hudson BD, Hovgaard CK, Milligan G, Ulven T (2012) Discovery of a potent and selective GPR120 agonist. J Med Chem 55:4511-4515
-
(2012)
J Med Chem
, vol.55
, pp. 4511-4515
-
-
Shimpukade, B.1
Hudson, B.D.2
Hovgaard, C.K.3
Milligan, G.4
Ulven, T.5
-
72
-
-
84930661586
-
Cloning and characterization of spliced variants of the porcine G protein coupled receptor 120
-
Song T, Peng J, Ren J, Wei HK, Peng J (2015) Cloning and characterization of spliced variants of the porcine G protein coupled receptor 120. Biomed Res Int 2015:813816
-
(2015)
Biomed Res Int
, vol.2015
, pp. 813816
-
-
Song, T.1
Peng, J.2
Ren, J.3
Wei, H.K.4
Peng, J.5
-
73
-
-
84974707326
-
GPR120 promotes adipogenesis through intracellular calcium and extracellular signal-regulated kinase 1/2 signal pathway
-
Song T, Zhou Y, Peng J, Tao YX, Yang Y, Xu T et al (2016) GPR120 promotes adipogenesis through intracellular calcium and extracellular signal-regulated kinase 1/2 signal pathway. Mol Cell Endocrinol 434:1-13
-
(2016)
Mol Cell Endocrinol
, vol.434
, pp. 1-13
-
-
Song, T.1
Zhou, Y.2
Peng, J.3
Tao, Y.X.4
Yang, Y.5
Xu, T.6
-
74
-
-
84902544474
-
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)
-
Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C et al (2014) Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett 24:3100-3103
-
(2014)
Bioorg Med Chem Lett
, vol.24
, pp. 3100-3103
-
-
Sparks, S.M.1
Chen, G.2
Collins, J.L.3
Danger, D.4
Dock, S.T.5
Jayawickreme, C.6
-
75
-
-
84901191678
-
GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans
-
Stone VM, Dhayal S, Brocklehurst KJ, Lenaghan C, Sorhede Winzell M, Hammar M et al (2014) GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans. Diabetologia 57:1182-1191
-
(2014)
Diabetologia
, vol.57
, pp. 1182-1191
-
-
Stone, V.M.1
Dhayal, S.2
Brocklehurst, K.J.3
Lenaghan, C.4
Sorhede Winzell, M.5
Hammar, M.6
-
76
-
-
84878888184
-
DC260126: A small-molecule antagonist of GPR40 that protects against pancreatic beta-Cells dysfunction in db/db mice
-
Sun P, Wang T, Zhou Y, Liu H, Jiang H, Zhu W et al (2013) DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic beta-Cells dysfunction in db/db mice. PLoS One 8, e66744
-
(2013)
Plos One
, vol.8
-
-
Sun, P.1
Wang, T.2
Zhou, Y.3
Liu, H.4
Jiang, H.5
Zhu, W.6
-
77
-
-
80052021813
-
Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases
-
Talukdar S, Olefsky JM, Osborn O (2011) Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases. Trends Pharmacol Sci 32:543-550
-
(2011)
Trends Pharmacol Sci
, vol.32
, pp. 543-550
-
-
Talukdar, S.1
Olefsky, J.M.2
Osborn, O.3
-
78
-
-
39149097541
-
Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening
-
Tikhonova IG, Sum CS, Neumann S, Engel S, Raaka BM, Costanzi S et al (2008) Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening. J Med Chem 51:625-633
-
(2008)
J Med Chem
, vol.51
, pp. 625-633
-
-
Tikhonova, I.G.1
Sum, C.S.2
Neumann, S.3
Engel, S.4
Raaka, B.M.5
Costanzi, S.6
-
79
-
-
84918779133
-
Tumor necrosis factor alpha decreases glucagon-like peptide-2 expression by up-regulating G-protein- coupled receptor 120 in Crohn disease
-
Tsukahara T, Watanabe K, Watanabe T, Yamagami H, Sogawa M, Tanigawa T et al (2015) Tumor necrosis factor alpha decreases glucagon-like peptide-2 expression by up-regulating G-protein- coupled receptor 120 in Crohn disease. Am J Pathol 185:185-196
-
(2015)
Am J Pathol
, vol.185
, pp. 185-196
-
-
Tsukahara, T.1
Watanabe, K.2
Watanabe, T.3
Yamagami, H.4
Sogawa, M.5
Tanigawa, T.6
-
80
-
-
84937576781
-
Dietary influences on regulation of the long-chain fatty acid receptor FFA4/GPR120
-
Ulven T, Christiansen E (2015) Dietary influences on regulation of the long-chain fatty acid receptor FFA4/GPR120. Annu Rev Nutr 35:239-263
-
(2015)
Annu Rev Nutr
, vol.35
, pp. 239-263
-
-
Ulven, T.1
Christiansen, E.2
-
81
-
-
33746589423
-
2 receptors DP and CRTH2 for treatment of inflammation
-
2 receptors DP and CRTH2 for treatment of inflammation. Curr Top Med Chem 6:1427-1444
-
(2006)
Curr Top Med Chem
, vol.6
, pp. 1427-1444
-
-
Ulven, T.1
Kostenis, E.2
-
82
-
-
84935859525
-
Discovery of a series of 2-(Pyridinyl)pyrimidines as potent antagonists of GPR40
-
Waring MJ, Baker DJ, Bennett SNL, Dossetter AG, Fenwick M, Garcia R et al (2015) Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR40. Med Chem Commun 6:1024-1029
-
(2015)
Med Chem Commun
, vol.6
, pp. 1024-1029
-
-
Waring, M.J.1
Baker, D.J.2
Bennett, S.3
Dossetter, A.G.4
Fenwick, M.5
Garcia, R.6
-
83
-
-
84859949278
-
Differential signaling by splice variants of the human free fatty acid receptor GPR120
-
Watson SJ, Brown AJ, Holliday ND (2012) Differential signaling by splice variants of the human free fatty acid receptor GPR120. Mol Pharmacol 81:631-642
-
(2012)
Mol Pharmacol
, vol.81
, pp. 631-642
-
-
Watson, S.J.1
Brown, A.J.2
Holliday, N.D.3
-
84
-
-
84874781809
-
The free fatty acid receptor G protein-coupled receptor 40 (GPR40) protects from bone loss through inhibition of osteoclast differentiation
-
Wauquier F, Philippe C, Leotoing L, Mercier S, Davicco MJ, Lebecque P et al (2013) The free fatty acid receptor G protein-coupled receptor 40 (GPR40) protects from bone loss through inhibition of osteoclast differentiation. J Biol Chem 288:6542-6551
-
(2013)
J Biol Chem
, vol.288
, pp. 6542-6551
-
-
Wauquier, F.1
Philippe, C.2
Leotoing, L.3
Mercier, S.4
Davicco, M.J.5
Lebecque, P.6
-
85
-
-
84897408840
-
Activation of the omega-3 fatty acid receptor GPR120 mediates anti-inflammatory actions in immortalized hypothalamic neurons
-
Wellhauser L, Belsham DD (2014) Activation of the omega-3 fatty acid receptor GPR120 mediates anti-inflammatory actions in immortalized hypothalamic neurons. J Neuroinflammation 11:60
-
(2014)
J Neuroinflammation
, vol.11
, pp. 60
-
-
Wellhauser, L.1
Belsham, D.D.2
-
86
-
-
77953722717
-
Probing the probes: Fitness factors for small molecule tools
-
Workman P, Collins I (2010) Probing the probes: fitness factors for small molecule tools. Chem Biol 17:561-577
-
(2010)
Chem Biol
, vol.17
, pp. 561-577
-
-
Workman, P.1
Collins, I.2
-
87
-
-
84890548520
-
Identification of G-protein-coupled receptor 120 as a tumor-promoting receptor that induces angiogenesis and migration in human colorectal carcinoma
-
Wu Q, Wang H, Zhao X, Shi Y, Jin M, Wan B et al (2013) Identification of G-protein-coupled receptor 120 as a tumor-promoting receptor that induces angiogenesis and migration in human colorectal carcinoma. Oncogene 32:5541-5550
-
(2013)
Oncogene
, vol.32
, pp. 5541-5550
-
-
Wu, Q.1
Wang, H.2
Zhao, X.3
Shi, Y.4
Jin, M.5
Wan, B.6
-
88
-
-
84879582536
-
Omega-3 fatty acids prevent inflammation and metabolic disorder through inhibition of NLRP3 inflammasome activation
-
Yan Y, Jiang W, Spinetti T, Tardivel A, Castillo R, Bourquin C et al (2013) Omega-3 fatty acids prevent inflammation and metabolic disorder through inhibition of NLRP3 inflammasome activation. Immunity 38:1154-1163
-
(2013)
Immunity
, vol.38
, pp. 1154-1163
-
-
Yan, Y.1
Jiang, W.2
Spinetti, T.3
Tardivel, A.4
Castillo, R.5
Bourquin, C.6
|