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Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
McClure, Kim F; Darout, Etzer; Guimarães, Cristiano R W; DeNinno, Michael P; Mascitti, Vincent; Munchhof, Michael J; Robinson, Ralph P; Kohrt, Jeffrey; Harris, Anthony R; Moore, Dianna E; Li, Bryan; Samp, Lacey; Lefker, Bruce A; Futatsugi, Kentaro; Kung, Daniel; Bonin, Paul D; Cornelius, Peter; Wang, Ruduan; Salter, Eben; Hornby, Sam; Kalgutkar, Amit S; Chen, Yue.
Affiliation
  • McClure KF; Department of Medicinal Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States. kim.f.mcclure@pfizer.com
J Med Chem ; 54(6): 1948-52, 2011 Mar 24.
Article in En | MEDLINE | ID: mdl-21361292
ABSTRACT
The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Receptors, G-Protein-Coupled / Azabicyclo Compounds Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2011 Document type: Article Affiliation country:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Receptors, G-Protein-Coupled / Azabicyclo Compounds Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2011 Document type: Article Affiliation country: