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GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Taylor, Alexander M; Bailey, Chris; Belmont, Lisa D; Campbell, Robert; Cantone, Nico; Côté, Alexandre; Crawford, Terry D; Cummings, Richard; DeMent, Kevin; Duplessis, Martin; Flynn, Megan; Good, Andrew C; Huang, Hon-Ren; Joshi, Shivangi; Leblanc, Yves; Murray, Jeremy; Nasveschuk, Christopher G; Neiss, Adrianne; Poy, Florence; Romero, F Anthony; Sandy, Peter; Tang, Yong; Tsui, Vickie; Zawadzke, Laura; Sims, Robert J; Audia, James E; Bellon, Steven F; Magnuson, Steven R; Albrecht, Brian K; Cochran, Andrea G.
Afiliação
  • Taylor AM; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Bailey C; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Belmont LD; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Campbell R; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cantone N; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Côté A; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Crawford TD; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Cummings R; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • DeMent K; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Duplessis M; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Flynn M; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Good AC; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Huang HR; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Joshi S; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Leblanc Y; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Murray J; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Nasveschuk CG; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Neiss A; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Poy F; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Romero FA; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Sandy P; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Tang Y; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Tsui V; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Zawadzke L; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Sims RJ; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Audia JE; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Bellon SF; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Magnuson SR; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
  • Albrecht BK; Constellation, a Morphosys Company, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
  • Cochran AG; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.
J Med Chem ; 65(16): 11177-11186, 2022 08 25.
Article em En | MEDLINE | ID: mdl-35930799
ABSTRACT
Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with acetyllysine, and therefore bromodomains have been targets for drug discovery efforts. Highly potent and selective ligands with good cellular permeability have been proposed as chemical probes for use in exploring the functions of many of the bromodomain proteins. We report here the discovery of a class of such inhibitors targeting the family VIII bromodomains of SMARCA2 (BRM) and SMARCA4 (BRG1), and PBRM1 (polybromo-1) bromodomain 5. We propose one example from this series, GNE-064, as a chemical probe for the bromodomains SMARCA2, SMARCA4, and PBRM1(5) with the potential for in vivo use.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fatores de Transcrição / DNA Helicases Limite: Humans Idioma: En Ano de publicação: 2022 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Fatores de Transcrição / DNA Helicases Limite: Humans Idioma: En Ano de publicação: 2022 Tipo de documento: Article