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

Autor:	Sha-Sha Cheng, Guan-Jun Yang, Wanhe Wang, Chung-Hang Leung, Dik-Lung Ma
Jazyk:	angličtina
Rok vydání:	2020
Předmět:	Protein-protein interaction Covalent inhibitors Cancer therapy Diseases of the blood and blood-forming organs RC633-647.5 Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Zdroj:	Journal of Hematology & Oncology, Vol 13, Iss 1, Pp 1-14 (2020)
Druh dokumentu:	article
ISSN:	1756-8722
DOI:	10.1186/s13045-020-00850-0
Popis:	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.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/e2d047b6c9634943a18bd1899f69e0c1 Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.