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Journal of Hematology & Oncology
Published in: Journal of Hematology & Oncology 1/2020

Open Access 01-12-2020 | Cancer Therapy | Review

The design and development of covalent protein-protein interaction inhibitors for cancer treatment

Authors: Sha-Sha Cheng, Guan-Jun Yang, Wanhe Wang, Chung-Hang Leung, Dik-Lung Ma

Published in: Journal of Hematology & Oncology | Issue 1/2020

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Abstract

Protein-protein interactions (PPIs) are central to a variety of biological processes, and their dysfunction is implicated in the pathogenesis of a range of human diseases, including cancer. Hence, the inhibition of PPIs has attracted significant attention in drug discovery. Covalent inhibitors have been reported to achieve high efficiency through forming covalent bonds with cysteine or other nucleophilic residues in the target protein. Evidence suggests that there is a reduced risk for the development of drug resistance against covalent drugs, which is a major challenge in areas such as oncology and infectious diseases. Recent improvements in structural biology and chemical reactivity have enabled the design and development of potent and selective covalent PPI inhibitors. In this review, we will highlight the design and development of therapeutic agents targeting PPIs for cancer therapy.
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Metadata
Title
The design and development of covalent protein-protein interaction inhibitors for cancer treatment
Authors
Sha-Sha Cheng
Guan-Jun Yang
Wanhe Wang
Chung-Hang Leung
Dik-Lung Ma
Publication date
01-12-2020
Publisher
BioMed Central
Keyword
Cancer Therapy
Published in
Journal of Hematology & Oncology / Issue 1/2020
Electronic ISSN: 1756-8722
DOI
https://doi.org/10.1186/s13045-020-00850-0

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