1. Baxter JD, Webb P. (2006) Metabolism: bile acids heat things up.
Nature, 439: 402-403.
[PMID:16437098]
2. de Oliveira MC, Gilglioni EH, de Boer BA, Runge JH, de Waart DR, Salgueiro CL, Ishii-Iwamoto EL, Oude Elferink RP, Gaemers IC. (2016) Bile acid receptor agonists INT747 and INT777 decrease oestrogen deficiency-related postmenopausal obesity and hepatic steatosis in mice.
Biochim Biophys Acta, 1862 (11): 2054-2062.
[PMID:27475255]
3. Genet C, Strehle A, Schmidt C, Boudjelal G, Lobstein A, Schoonjans K, Souchet M, Auwerx J, Saladin R, Wagner A. (2010) Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.
J Med Chem, 53 (1): 178-90.
[PMID:19911773]
4. Guo C, Chen WD, Wang YD. (2016) TGR5, Not Only a Metabolic Regulator.
Front Physiol, 7: 646.
[PMID:28082913]
5. Guo C, Xie S, Chi Z, Zhang J, Liu Y, Zhang L, Zheng M, Zhang X, Xia D, Ke Y et al.. (2016) Bile Acids Control Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome.
Immunity, 45 (4): 802-816.
[PMID:27692610]
6. Högenauer K, Arista L, Schmiedeberg N, Werner G, Jaksche H, Bouhelal R, Nguyen DG, Bhat BG, Raad L, Rauld C et al.. (2014) G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonists reduce the production of proinflammatory cytokines and stabilize the alternative macrophage phenotype.
J Med Chem, 57 (24): 10343-54.
[PMID:25411721]
7. Katsuma S, Hirasawa A, Tsujimoto G. (2005) Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1.
Biochem Biophys Res Commun, 329 (1): 386-90.
[PMID:15721318]
8. Kawamata Y, Fujii R, Hosoya M, Harada M, Yoshida H, Miwa M, Fukusumi S, Habata Y, Itoh T, Shintani Y, Hinuma S, Fujisawa Y, Fujino M. (2003) A G protein-coupled receptor responsive to bile acids.
J Biol Chem, 278: 9435-9440.
[PMID:12524422]
9. Li B, Yang N, Li C, Li C, Gao K, Xie X, Dong X, Yang J, Yang Q, Tong Z et al.. (2018) INT-777, a bile acid receptor agonist, extenuates pancreatic acinar cells necrosis in a mouse model of acute pancreatitis.
Biochem Biophys Res Commun, 503 (1): 38-44.
[PMID:29859191]
10. Maruyama T, Miyamoto Y, Nakamura T, Tamai Y, Okada H, Sugiyama E, Nakamura T, Itadani H, Tanaka K. (2002) Identification of membrane-type receptor for bile acids (M-BAR).
Biochem Biophys Res Commun, 298 (5): 714-9.
[PMID:12419312]
11. Pellicciari R, Gioiello A, Macchiarulo A, Thomas C, Rosatelli E, Natalini B, Sardella R, Pruzanski M, Roda A, Pastorini E et al.. (2009) Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
J Med Chem, 52 (24): 7958-61.
[PMID:20014870]
12. Picon S, Boulahjar R, Hoguet V, Baron M, Duplan I, Vallez E, Hennuyer N, Dumont J, Touche V, Dorchies E et al.. (2023) Discovery, Structure-Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5.
J Med Chem, 66 (17): 11732-11760.
[PMID:37639383]
13. Pols TW, Nomura M, Harach T, Lo Sasso G, Oosterveer MH, Thomas C, Rizzo G, Gioiello A, Adorini L, Pellicciari R et al.. (2011) TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading.
Cell Metab, 14 (6): 747-57.
[PMID:22152303]
14. Rizzo G, Passeri D, De Franco F, Ciaccioli G, Donadio L, Rizzo G, Orlandi S, Sadeghpour B, Wang XX, Jiang T et al.. (2010) Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist.
Mol Pharmacol, 78 (4): 617-30.
[PMID:20631053]
15. Sato H, Genet C, Strehle A, Thomas C, Lobstein A, Wagner A, Mioskowski C, Auwerx J, Saladin R. (2007) Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea.
Biochem Biophys Res Commun, 362 (4): 793-8.
[PMID:17825251]
16. Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S. (2002) Identification of G protein-coupled receptor genes from the human genome sequence.
FEBS Lett, 520 (1-3): 97-101.
[PMID:12044878]
17. Wang XX, Edelstein MH, Gafter U, Qiu L, Luo Y, Dobrinskikh E, Lucia S, Adorini L, D'Agati VD, Levi J et al.. (2016) G Protein-Coupled Bile Acid Receptor TGR5 Activation Inhibits Kidney Disease in Obesity and Diabetes.
J Am Soc Nephrol, 27 (5): 1362-78.
[PMID:26424786]
18. Watanabe M, Houten SM, Mataki C, Christoffolete MA, Kim BW, Sato H, Messaddeq N, Harney JW, Ezaki O, Kodama T et al.. (2006) Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation.
Nature, 439 (7075): 484-9.
[PMID:16400329]
19. Yun Y, Zhang C, Guo S, Liang X, Lan Y, Wang M, Zhuo N, Yin J, Liu H, Gu M et al.. (2021) Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5H88Y Mutant Mice.
J Med Chem, 64 (16): 12181-12199.
[PMID:34406006]