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.
CITE THIS COLLECTION
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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Alexander M. Taylor
Lisa D. Belmont
Terry D. Crawford
Andrew C. Good
Christopher G. Nasveschuk
F. Anthony Romero