Bioorganic & Medicinal Chemistry Letters 2007-09-01

Agonist lead identification for the high affinity niacin receptor GPR109a.

Tawfik Gharbaoui, Philip J Skinner, Young-Jun Shin, Claudia Averbuj, Jae-Kyu Jung, Benjamin R Johnson, Tracy Duong, Marc Decaire, Jane Uy, Martin C Cherrier, Peter J Webb, Susan Y Tamura, Ning Zou, Nathalie Rodriguez, P Douglas Boatman, Carleton R Sage, Andrew Lindstrom, Jerry Xu, Thomas O Schrader, Brian M Smith, Ruoping Chen, Jeremy G Richman, Daniel T Connolly, Steven L Colletti, James R Tata, Graeme Semple

文献索引：Bioorg. Med. Chem. Lett. 17 , 4914-9, (2007)

全文：HTML全文

摘要

A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.

相关化合物

  • 烟酸
  • 5-溴烟酸

相关文献：

1,25-dihydroxyvitamin D3 causes ADAM10-dependent ectodomain shedding of tumor necrosis factor receptor 1 in vascular smooth muscle cells.

2015-01-01

[Mol. Pharmacol. 87(3) , 533-42, (2015)]

Evidence for fatty acids mediating CL 316,243-induced reductions in blood glucose in mice.

2014-10-01

[Am. J. Physiol. Endocrinol. Metab. 307(7) , E563-70, (2014)]

Protein enrichment of an Opuntia ficus-indica cladode hydrolysate by cultivation of Candida utilis and Kluyveromyces marxianus.

2015-03-30

[J. Sci. Food Agric. 95(5) , 1094-102, (2015)]

Effect of concentrate feeder design on performance, eating and animal behavior, welfare, ruminal health, and carcass quality in Holstein bulls fed high-concentrate diets.

2015-06-01

[J. Anim. Sci. 93 , 3018-33, (2015)]

Solubilization of gliadins for use as a source of nitrogen in the selection of bacteria with gliadinase activity.

2015-02-01

[Food Chem. 168 , 439-44, (2014)]

更多文献...