-
1
-
-
0036432845
-
Identification of membrane-type receptor for bile acids (M-BAR)
-
Maruyama, T. et al. Identification of membrane-type receptor for bile acids (M-BAR). Biochem. Biophys. Res. Commun. 298, 714-719 (2002).
-
(2002)
Biochem. Biophys. Res. Commun.
, vol.298
, pp. 714-719
-
-
Maruyama, T.1
-
2
-
-
0003269455
-
A G protein-coupled receptor responsive to bile acids
-
Kawamata, Y. et al. A G protein-coupled receptor responsive to bile acids. J. Biol. Chem. 278, 9435-9440 (2003).
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 9435-9440
-
-
Kawamata, Y.1
-
3
-
-
79959525960
-
The bile acid membrane receptor TGR5: A valuable metabolic target
-
Pols, T. W., Noriega, L. G., Nomura, M., Auwerx, J. & Schoonjans, K. The bile acid membrane receptor TGR5: a valuable metabolic target. Dig. Dis. 29, 37-44 (2011).
-
(2011)
Dig. Dis.
, vol.29
, pp. 37-44
-
-
Pols, T.W.1
Noriega, L.G.2
Nomura, M.3
Auwerx, J.4
Schoonjans, K.5
-
4
-
-
78649386642
-
The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain
-
Keitel, V. et al. The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain. Glia 58, 1794-1805 (2010).
-
(2010)
Glia
, vol.58
, pp. 1794-1805
-
-
Keitel, V.1
-
5
-
-
33748757234
-
Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation
-
Vassileva, G. et al. Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation. Biochem. J. 398, 423-430 (2006).
-
(2006)
Biochem. J.
, vol.398
, pp. 423-430
-
-
Vassileva, G.1
-
6
-
-
13844299425
-
Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1
-
Katsuma, S., Hirasawa, A. & Tsujimoto, G. Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1. Biochem. Biophys. Res. Commun. 329, 386-390 (2005).
-
(2005)
Biochem. Biophys. Res. Commun.
, vol.329
, pp. 386-390
-
-
Katsuma, S.1
Hirasawa, A.2
Tsujimoto, G.3
-
7
-
-
84857772149
-
The structure and function of the glucagon-like peptide-1 receptor and its ligands
-
Donnelly, D. The structure and function of the glucagon-like peptide-1 receptor and its ligands. Br. J. Pharmacol. 166, 27-41 (2012).
-
(2012)
Br. J. Pharmacol.
, vol.166
, pp. 27-41
-
-
Donnelly, D.1
-
8
-
-
69149083245
-
TGR5-mediated bile acid sensing controls glucose homeostasis
-
Thomas, C. et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 10, 167-177 (2009).
-
(2009)
Cell Metab.
, vol.10
, pp. 167-177
-
-
Thomas, C.1
-
9
-
-
31444454037
-
Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation
-
Watanabe, M. et al. Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 439, 484-489 (2006).
-
(2006)
Nature
, vol.439
, pp. 484-489
-
-
Watanabe, M.1
-
10
-
-
80052720863
-
TGR5: A novel target for weight maintenance and glucose metabolism
-
Chen, X., Lou, G., Meng, Z. & Huang, W. TGR5: a novel target for weight maintenance and glucose metabolism. Exp. Diabetes Res. 2011, 853501 (2011).
-
(2011)
Exp. Diabetes Res.
, vol.2011
, pp. 853501
-
-
Chen, X.1
Lou, G.2
Meng, Z.3
Huang, W.4
-
11
-
-
79956088562
-
The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation
-
Pols, T. W., Noriega, L. G., Nomura, M., Auwerx, J. & Schoonjans, K. The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation. J. Hepatol. 54, 1263-1272 (2011).
-
(2011)
J. Hepatol.
, vol.54
, pp. 1263-1272
-
-
Pols, T.W.1
Noriega, L.G.2
Nomura, M.3
Auwerx, J.4
Schoonjans, K.5
-
12
-
-
77949425951
-
TGR5 as a therapeutic target for treating obesity
-
Zhong, M. TGR5 as a therapeutic target for treating obesity. Curr. Top. Med. Chem. 10, 386-396 (2010).
-
(2010)
Curr. Top. Med. Chem.
, vol.10
, pp. 386-396
-
-
Zhong, M.1
-
13
-
-
73249134773
-
Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists
-
Evans, K. A. et al. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J. Med. Chem. 52, 7962-7965 (2009).
-
(2009)
J. Med. Chem.
, vol.52
, pp. 7962-7965
-
-
Evans, K.A.1
-
14
-
-
84943222848
-
Novel small molecule agonist of TGR5 possesses anti-diabetic effects but causes gallbladder filling in mice
-
Briere, D. A. et al. Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice. PloS One 10, e0136873 (2015).
-
(2015)
PloS One
, vol.10
, pp. e0136873
-
-
Briere, D.A.1
-
15
-
-
84899516119
-
Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: Structure-activity relationships, lead optimization and chronic in vivo efficacy
-
Phillips, D. P. et al. Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization and chronic in vivo efficacy. J. Med. Chem. 57, 3263-3282 (2014).
-
(2014)
J. Med. Chem.
, vol.57
, pp. 3263-3282
-
-
Phillips, D.P.1
-
16
-
-
84875609906
-
2-Phenoxy-nicotinamides are potent agonists at the bile acid receptor GPBAR1 (TGR5)
-
Martin, R. E. et al. 2-Phenoxy-nicotinamides are potent agonists at the bile acid receptor GPBAR1 (TGR5). Chem Med Chem 8, 569-576 (2013).
-
(2013)
Chem Med Chem
, vol.8
, pp. 569-576
-
-
Martin, R.E.1
-
17
-
-
84955454063
-
Discovery of a potent and orally efficacious TGR5 receptor agonist
-
Agarwal, S. et al. Discovery of a potent and orally efficacious TGR5 receptor agonist. ACS Med. Chem. Lett. 7, 51-55 (2016).
-
(2016)
ACS Med. Chem. Lett.
, vol.7
, pp. 51-55
-
-
Agarwal, S.1
-
18
-
-
84896730426
-
G protein-coupled bile acid receptor 1 stimulation mediates arterial vasodilation through a K(Ca)1.1 (BK(Ca))- dependent mechanism
-
Fryer, R. M. et al. G protein-coupled bile acid receptor 1 stimulation mediates arterial vasodilation through a K(Ca)1.1 (BK(Ca))- dependent mechanism. J. Pharmacol. Exp. Ther. 348, 421-431 (2014).
-
(2014)
J. Pharmacol. Exp. Ther.
, vol.348
, pp. 421-431
-
-
Fryer, R.M.1
-
19
-
-
79957663467
-
The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling
-
Li, T. et al. The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling. Mol. Endocrinol. 25, 1066-1071 (2011).
-
(2011)
Mol. Endocrinol.
, vol.25
, pp. 1066-1071
-
-
Li, T.1
-
20
-
-
84870976388
-
Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists
-
Duan, H. et al. Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J. Med. Chem. 55, 10475-10489 (2012).
-
(2012)
J. Med. Chem.
, vol.55
, pp. 10475-10489
-
-
Duan, H.1
-
21
-
-
84872285850
-
Identification of tetrahydropyrido[4,3-d]pyrimidine Amides as a new class of orally bioavailable TGR5 agonists
-
Piotrowski, D. W. et al. Identification of tetrahydropyrido[4,3-d]pyrimidine Amides as a new class of orally bioavailable TGR5 agonists. ACS Med. Chem. Lett. 4, 63-68 (2013).
-
(2013)
ACS Med. Chem. Lett.
, vol.4
, pp. 63-68
-
-
Piotrowski, D.W.1
-
22
-
-
84871791175
-
Optimization of triazole-based TGR5 agonists towards orally available agents
-
Futatsugi, K. et al. Optimization of triazole-based TGR5 agonists towards orally available agents. Med Chem Comm 4, 205-210 (2013).
-
(2013)
Med Chem Comm
, vol.4
, pp. 205-210
-
-
Futatsugi, K.1
-
23
-
-
84975700732
-
Recent progress on bile acid receptor modulators for treatment of metabolic diseases
-
Xu, Y. Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases. J. Med. Chem. doi: 10.1021/acs. jmedchem.5b00342 (2016).
-
(2016)
J. Med. Chem.
-
-
Xu, Y.1
-
24
-
-
84960880692
-
The therapeutic potential of TGR5 agonists. Hope or hype?
-
Hodge, R. J. & Nunez, D. J. The Therapeutic Potential of TGR5 Agonists. Hope or Hype? Diabetes Obes. Metab. doi: 10.1111/dom.12636 (2016).
-
(2016)
Diabetes Obes. Metab.
-
-
Hodge, R.J.1
Nunez, D.J.2
-
25
-
-
84928501244
-
Discovery of intestinal targeted TGR5 agonists for the treatment of type 2 diabetes
-
Duan, H. et al. Discovery of intestinal targeted TGR5 agonists for the treatment of type 2 diabetes. J. Med. Chem. 58, 3315-3328 (2015).
-
(2015)
J. Med. Chem.
, vol.58
, pp. 3315-3328
-
-
Duan, H.1
-
26
-
-
79959785811
-
Role of bile acid sequestrants in the treatment of type 2 diabetes
-
Handelsman, Y. Role of bile acid sequestrants in the treatment of type 2 diabetes. Diabetes Care 34 Suppl 2, S244-250 (2011).
-
(2011)
Diabetes Care
, vol.34
, pp. S244-250
-
-
Handelsman, Y.1
-
27
-
-
84909988804
-
Lipid-lowering agents in the management of nonalcoholic fatty liver disease
-
Tziomalos, K. Lipid-lowering agents in the management of nonalcoholic fatty liver disease. World J. Hepatol. 6, 738-744 (2014).
-
(2014)
World J. Hepatol.
, vol.6
, pp. 738-744
-
-
Tziomalos, K.1
-
28
-
-
84895775124
-
Bile acid sequestrants: Glucose-lowering mechanisms and efficacy in type 2 diabetes
-
Hansen, M., Sonne, D. P. & Knop, F. K. Bile acid sequestrants: glucose-lowering mechanisms and efficacy in type 2 diabetes. Curr. Diab. Rep. 14, 482-490 (2014).
-
(2014)
Curr. Diab. Rep.
, vol.14
, pp. 482-490
-
-
Hansen, M.1
Sonne, D.P.2
Knop, F.K.3
-
29
-
-
84861682490
-
TGR5 potentiates GLP-1 secretion in response to anionic exchange resins
-
Harach, T. et al. TGR5 potentiates GLP-1 secretion in response to anionic exchange resins. Sci. Rep. 2, 430-436 (2012).
-
(2012)
Sci. Rep.
, vol.2
, pp. 430-436
-
-
Harach, T.1
-
30
-
-
84899482356
-
Glucose-lowering effects of intestinal bile acid sequestration through enhancement of splanchnic glucose utilization
-
Prawitt, J., Caron, S. & Staels, B. Glucose-lowering effects of intestinal bile acid sequestration through enhancement of splanchnic glucose utilization. Trends Endocrinol. Metab. 25, 235-244 (2014).
-
(2014)
Trends Endocrinol. Metab.
, vol.25
, pp. 235-244
-
-
Prawitt, J.1
Caron, S.2
Staels, B.3
-
31
-
-
84875200057
-
-
Patent Cooperation Treaty (PCT) WO2011071565A1. Jun 16
-
Boliu, V. et al. Inventors; Exelixis, Inc., assignee. TGR5 agonists. Patent Cooperation Treaty (PCT) WO2011071565A1. 2011 Jun 16.
-
(2011)
TGR5 Agonists
-
-
Boliu, V.1
|