Optimized Chemical Probes for REV-ERBα

REV-ERBα has emerged as an important target for regulation of circadian rhythm and its associated physiology. Herein, we report on the optimization of a series of REV-ERBα agonists based on GSK4112 (1) for potency, selectivity, and bioavailability. Potent REV-ERBα agonists 4, 10, 16, and 23 are deta...

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Pubblicato in:J Med Chem
Autori principali: Trump, Ryan P., Bresciani, Stefano, Cooper, Anthony W. J., Tellam, James P., Wojno, Justyna, Blaikley, John, Orband-Miller, Lisa A., Kashatus, Jennifer A., Dawson, Helen C., Loudon, Andrew, Ray, David, Grant, Daniel, Farrow, Stuart N., Willson, Timothy M., Tomkinson, Nicholas C. O.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2013
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4347663/
https://ncbi.nlm.nih.gov/pubmed/23656296
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm400458q
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