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Bioorg Med Chem Lett. 2012 Jul 1;22(13):4413-7. doi: 10.1016/j.bmcl.2012.04.126. Epub 2012 May 8.

Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.

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  • 1Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.

Abstract

The structure-activity relationship study of a small molecule Rev-erbα agonist is reported. The potency and efficacy of the agonists in a cell-based assay were optimized as compared to the initial lead. Modest mouse pharmacokinetics coupled with an improved in vitro profile make 12e a suitable in vivo probe to interrogate the functions of Rev-erbα in animal models of disease.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
22633688
[PubMed - indexed for MEDLINE]
PMCID:
PMC3376186
Free PMC Article
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