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Volumn 6, Issue , 2016, Pages

Intestinally-targeted TGR5 agonists equipped with quaternary ammonium have an improved hypoglycemic effect and reduced gallbladder filling effect

Author keywords

[No Author keywords available]

Indexed keywords

AMMONIUM DERIVATIVE; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR; GLUCAGON LIKE PEPTIDE 1; GPBAR1 PROTEIN, HUMAN; GPBAR1 PROTEIN, MOUSE; QUATERNARY AMMONIUM DERIVATIVE;

EID: 84975760202     PISSN: None     EISSN: 20452322     Source Type: Journal    
DOI: 10.1038/srep28676     Document Type: Article
Times cited : (50)

References (33)
  • 1
    • 0036432845 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.