Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.

[1]  J. Auwerx,et al.  Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes. , 2010, Journal of medicinal chemistry.

[2]  J. Auwerx,et al.  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. , 2009, Journal of medicinal chemistry.

[3]  K. Evans,et al.  Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. , 2009, Journal of medicinal chemistry.

[4]  A. Tiwari,et al.  TGR5: an emerging bile acid G-protein-coupled receptor target for the potential treatment of metabolic disorders. , 2009, Drug discovery today.

[5]  Johan Auwerx,et al.  Targeting bile-acid signalling for metabolic diseases , 2008, Nature Reviews Drug Discovery.

[6]  J. Auwerx,et al.  Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. , 2008, Journal of medicinal chemistry.

[7]  J. Auwerx,et al.  Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea. , 2007, Biochemical and biophysical research communications.

[8]  J. Auwerx,et al.  Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5. , 2007, Journal of medicinal chemistry.

[9]  H. Miyoshi,et al.  Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice. , 2006, The Journal of endocrinology.

[10]  H. Davis,et al.  Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation. , 2006, The Biochemical journal.

[11]  A. Groen.  The emerging role of bile acids as integrators of intermediary metabolism. , 2006, Journal of hepatology.

[12]  J. Auwerx,et al.  Endocrine functions of bile acids , 2006, The EMBO journal.

[13]  J. Auwerx,et al.  Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation , 2006, Nature.

[14]  G. Tsujimoto,et al.  Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1. , 2005, Biochemical and biophysical research communications.

[15]  Masataka Harada,et al.  A G Protein-coupled Receptor Responsive to Bile Acids* , 2003, The Journal of Biological Chemistry.

[16]  Takao Nakamura,et al.  Identification of membrane-type receptor for bile acids (M-BAR). , 2002, Biochemical and biophysical research communications.

[17]  M. Makishima,et al.  Identification of a nuclear receptor for bile acids. , 1999, Science.