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. |
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| 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 |
| FullText | Text: Availability: 0 |
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| Header | DbId: mdl DbLabel: MEDLINE Ultimate An: 41432990 AccessLevel: 2 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: 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. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AU" term="%22Maram+L%22">Maram L</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Valfort+AC%22">Valfort AC</searchLink>; Department of Cellular and Systems Pharmacology, University of Florida College of Pharmacy, Gainesville, Florida 32610, United States.<br /><searchLink fieldCode="AU" term="%22Homaidur+Rahman+M%22">Homaidur Rahman M</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Okda+HE%22">Okda HE</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Elagawany+M%22">Elagawany M</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Politte+H%22">Politte H</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Appourchaux+K%22">Appourchaux K</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Bedia-Diaz+G%22">Bedia-Diaz G</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Côté+I%22">Côté I</searchLink>; Department of Cellular and Systems Pharmacology, University of Florida College of Pharmacy, Gainesville, Florida 32610, United States.<br /><searchLink fieldCode="AU" term="%22Hegazy+L%22">Hegazy L</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Burris+TP%22">Burris TP</searchLink>; 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.<br /><searchLink fieldCode="AU" term="%22Elgendy+B%22">Elgendy B</searchLink>; 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. – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2026 Jan 08; Vol. 69 (1), pp. 439-465. <i>Date of Electronic Publication: </i>2025 Dec 23. – Name: TypePub Label: Publication Type Group: TypPub Data: Journal Article – Name: TitleSource Label: Journal Info Group: Src Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>9716531 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1520-4804 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2200222623%22">00222623 </searchLink><i>NLM ISO Abbreviation: </i>J Med Chem <i>Subsets: </i>MEDLINE |
| PLink | https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=mdl&AN=41432990 |
| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1021/acs.jmedchem.5c02749 Languages: – Code: eng Text: English PhysicalDescription: Pagination: StartPage: 439 Titles: – TitleFull: 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. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Maram L – PersonEntity: Name: NameFull: Valfort AC – PersonEntity: Name: NameFull: Homaidur Rahman M – PersonEntity: Name: NameFull: Okda HE – PersonEntity: Name: NameFull: Elagawany M – PersonEntity: Name: NameFull: Politte H – PersonEntity: Name: NameFull: Appourchaux K – PersonEntity: Name: NameFull: Bedia-Diaz G – PersonEntity: Name: NameFull: Côté I – PersonEntity: Name: NameFull: Hegazy L – PersonEntity: Name: NameFull: Burris TP – PersonEntity: Name: NameFull: Elgendy B IsPartOfRelationships: – BibEntity: Dates: – D: 08 M: 01 Text: 2026 Jan 08 Type: published Y: 2026 Identifiers: – Type: issn-electronic Value: 1520-4804 Numbering: – Type: volume Value: 69 – Type: issue Value: 1 Titles: – TitleFull: Journal of medicinal chemistry Type: main |
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