GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1

Posted on 05.08.2022 - 21:20
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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Taylor, Alexander M.; Bailey, Chris; Belmont, Lisa D.; Campbell, Robert; Cantone, Nico; Côté, Alexandre; et al. (2022): GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. ACS Publications. Collection. https://doi.org/10.1021/acs.jmedchem.2c00662
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Journal of Medicinal Chemistry

AUTHORS (30)

Alexander M. Taylor
Chris Bailey
Lisa D. Belmont
Robert Campbell
Nico Cantone
Alexandre Côté
Terry D. Crawford
Richard Cummings
Kevin DeMent
Martin Duplessis
Megan Flynn
Andrew C. Good
Hon-Ren Huang
Shivangi Joshi
Yves Leblanc
Jeremy Murray
Christopher G. Nasveschuk
Adrianne Neiss
Florence Poy
F. Anthony Romero
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