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Discovery of BE2012, a First-in-Class REV-ERBα/β Antagonist with Favorable Selectivity and Pharmacokinetics, and In Vivo Efficacy in Inducing Key Myogenic Factors for Muscle Repair upon Acute Muscle Injury.

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Title: Discovery of BE2012, a First-in-Class REV-ERBα/β Antagonist with Favorable Selectivity and Pharmacokinetics, and In Vivo Efficacy in Inducing Key Myogenic Factors for Muscle Repair upon Acute Muscle Injury.
Authors: Maram L; Department of Anesthesiology, Washington University in St. Louis, St. Louis, Missouri 63110, United States.; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Valfort AC; Department of Cellular and Systems Pharmacology, University of Florida College of Pharmacy, Gainesville, Florida 32610, United States., Homaidur Rahman M; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Okda HE; Department of Anesthesiology, Washington University in St. Louis, St. Louis, Missouri 63110, United States.; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Elagawany M; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Politte H; Department of Anesthesiology, Washington University in St. Louis, St. Louis, Missouri 63110, United States.; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Appourchaux K; Department of Anesthesiology, Washington University in St. Louis, St. Louis, Missouri 63110, United States.; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Bedia-Diaz G; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Côté I; Department of Cellular and Systems Pharmacology, University of Florida College of Pharmacy, Gainesville, Florida 32610, United States., Hegazy L; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States., Burris TP; Department of Cellular and Systems Pharmacology, University of Florida College of Pharmacy, Gainesville, Florida 32610, United States.; University of Florida Genetics Institute, University of Florida School of Medicine, Gainesville, Florida 32610, United States., Elgendy B; Department of Anesthesiology, Washington University in St. Louis, St. Louis, Missouri 63110, United States.; Center for Clinical Pharmacology, Washington University School of Medicine and University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.; Department of Pharmaceutical and Administrative Sciences, University of Health Sciences and Pharmacy, St. Louis, Missouri 63110, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2026 Jan 08; Vol. 69 (1), pp. 439-465. Date of Electronic Publication: 2025 Dec 23.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.5c02749