- Agonist lead identification for the high affinity niacin receptor GPR109a.
Agonist lead identification for the high affinity niacin receptor GPR109a.
Bioorganic & medicinal chemistry letters (2007-06-26)
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
PMID17588745
RÉSUMÉ
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.
MATÉRIAUX
Référence du produit
Marque
Description du produit
Sigma-Aldrich
Acide nicotinique, BioReagent, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥98%