Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity-Reference-Cited by-同舟云学术

Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity

Published:2022-07-22 Issue:15 Volume:65 Page:10441-10458
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Guan Xianghong¹^ORCID,Cheryala Narsihmulu¹,Karim Rezaul Md.²^ORCID,Chan Alice²,Berndt Norbert²,Qi Jun³,Georg Gunda I.¹^ORCID,Schönbrunn Ernst²^ORCID

Affiliation:

1. Department of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street, Minneapolis, Minnesota 55414, United States

2. Moffitt Cancer Center, Drug Discovery Department, 12902 Magnolia Drive, Tampa, Florida 33612, United States

3. Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States

Funder

Eunice Kennedy Shriver National Institute of Child Health and Human Development

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.2c00453

Reference50 articles.

1. Targeting epigenetic reader domains by chemical biology

2. Bromodomains: a new target class for drug development

3. Targeting bromodomains: epigenetic readers of lysine acetylation

4. Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

5. Bromodomain biology and drug discovery

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