Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds-Reference-Cited by-同舟云学术

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Published:2017-06-22 Issue:2 Volume:61 Page:504-513
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Chan Kwok-Ho¹,Zengerle Michael¹,Testa Andrea¹,Ciulli Alessio¹^ORCID

Affiliation:

1. Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dow Street, Dundee, DD1 5EH, Scotland, U.K.

Funder

H2020 Marie Sklodowska-Curie Actions

Wellcome Trust

FP7 Ideas: European Research Council

Biotechnology and Biological Sciences Research Council

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

http://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.6b01912

Reference38 articles.

1. Drugging the undruggables: exploring the ubiquitin system for drug development

2. Induced protein degradation: an emerging drug discovery paradigm

3. Chemical approaches to targeted protein degradation through modulation of the ubiquitin–proteasome pathway

4. Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy

5. Structural basis of PROTAC cooperative recognition for selective protein degradation

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