Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine-Reference-Cited by-同舟云学术

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Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine

Published:2018-08-30 Issue:18 Volume:61 Page:8202-8211
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Kharenko Olesya A.¹^ORCID,Patel Reena G.¹,Brown S. David¹,Calosing Cyrus¹,White Andre²,Lakshminarasimhan Damodharan²,Suto Robert K.²,Duffy Bryan C.³,Kitchen Douglas B.³,McLure Kevin G.¹,Hansen Henrik C.¹,van der Horst Edward H.¹,Young Peter R.¹

Affiliation:

1. Zenith Epigenetics, Suite 300, 4820 Richard Road SW, Calgary, Alberta T3E 6L1, Canada

2. Xtal BioStructures, Inc., 12 Michigan Drive, Natick, Massachusetts 01760, United States

3. AMRI, 26 Corporate Circle, P.O. Box 15098, Albany, New York 12212-5098, United States

Funder

Zenith Epigenetics Ltd.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.8b00666

Reference22 articles.

1. The bromodomain interaction module

2. Targeting bromodomains: epigenetic readers of lysine acetylation

3. BET inhibitors: a novel epigenetic approach

4. The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

5. Novel approaches to targeting BRD4

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3. Development of covalent inhibitors: Principle, design, and application in cancer;MedComm – Oncology;2023-10-31

4. Recent progress and structural analyses of domain‐selective BET inhibitors;Medicinal Research Reviews;2023-03-27

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