Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction-Reference-Cited by-同舟云学术

Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction

Published:2023 Issue:9 Volume:14 Page:1803-1816
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Bum-Erdene Khuchtumur¹^ORCID,Ghozayel Mona K.¹^ORCID,Zhang Mark J.¹^ORCID,Gonzalez-Gutierrez Giovanni²^ORCID,Meroueh Samy O.¹^ORCID

Affiliation:

1. Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, 635 Barnhill Drive, MS4021, Indianapolis, Indiana, 46202, USA

2. Department of Molecular and Cellular Biochemistry, Indiana University, 212 S Hawthorne Drive, Bloomington, IN 47405, USA

Abstract

Screening of reactive chloroacetamide fragments yields covalent allosteric inhibitors of TEAD binding to YAP1. Follow-up time- and concentration-dependent characterization of novel inhibitor scaffolds is reported.

Funder

Vera Bradley Foundation for Breast Cancer

U.S. Department of Veterans Affairs

National Institutes of Health

American Cancer Society

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/MD/D3MD00264K

Reference48 articles.

1. Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD⋅Yap Protein-Protein Interaction

2. Effect of the acylation of TEAD4 on its interaction with co-activators YAP and TAZ

3. YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers

4. Genome-wide Association of Yorkie with Chromatin and Chromatin-Remodeling Complexes

5. TEAD mediates YAP-dependent gene induction and growth control

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