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

Taylor, Alexander M.; Bailey, Chris; Belmont, Lisa D.; Campbell, Robert; Cantone, Nico; Cote, 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 III, Robert J.; Audia, James E.; Bellon, Steven F.; Magnuson, Steven R.; Albrecht, Brian K.; Cochran, Andrea G.

doi:10.1021/acs.jmedchem.2c00662

Title: GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2

Journal Article · 01 August 2022 · J. Med. Chem.

DOI:https://doi.org/10.1021/acs.jmedchem.2c00662· OSTI ID:1900806

Taylor, Alexander M.; Bailey, Chris; Belmont, Lisa D.; Campbell, Robert; Cantone, Nico; Cote, 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 more »

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Research Organization:: Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)

Sponsoring Organization:: DOE - Office Of Science; INDUSTRY

OSTI ID:: 1900806

Journal Information:: J. Med. Chem., Vol. 65, Issue (16)

Country of Publication:: United States

Language:: ENGLISH

References (31)

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Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis Myrianthopoulos, Vassilios; Gaboriaud-Kolar, Nicolas; Tallant, Cynthia Journal of Medicinal Chemistry, Vol. 59, Issue 19 https://doi.org/10.1021/acs.jmedchem.6b00355	journal	September 2016
Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex Sutherell, Charlotte L.; Tallant, Cynthia; Monteiro, Octovia P. Journal of Medicinal Chemistry, Vol. 59, Issue 10 https://doi.org/10.1021/acs.jmedchem.5b01997	journal	May 2016
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The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies Vangamudi, Bhavatarini; Paul, Thomas A.; Shah, Parantu K. Cancer Research, Vol. 75, Issue 18 https://doi.org/10.1158/0008-5472.CAN-14-3798	journal	July 2015
The Bromodomains of the mammalian SWI/SNF (mSWI/SNF) ATPases Brahma (BRM) and Brahma Related Gene 1 (BRG1) promote chromatin interaction and are critical for skeletal muscle differentiation Sharma, Tapan; Robinson, Daniel C. L.; Witwicka, Hanna Nucleic Acids Research, Vol. 49, Issue 14 https://doi.org/10.1093/nar/gkab617	journal	July 2021

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