| Literature DB >> 21354793 |
Michael M-C Lo1, Harry R Chobanian, Oksana Palyha, Yanqing Kan, Theresa M Kelly, Xiao-Ming Guan, Marc L Reitman, Jasminka Dragovic, Kathryn A Lyons, Ravi P Nargund, Linus S Lin.
Abstract
Bombesin receptor subtype-3 (BRS-3) is an orphan G-protein coupled receptor belonging to the subfamily of bombesin-like receptors. BRS-3 is implicated in the development of obesity and diabetes. We report here small-molecule agonists that are based on a 4-(alkylamino)pyridine-3-sulfonamide core. We describe the discovery of 2a, which has mid-nanomolar potency, selectivity for human BRS-3 versus the other bombesin-like receptors, and good bioavailability.Entities:
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Year: 2011 PMID： 21354793 DOI： 10.1016/j.bmcl.2011.02.011
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823