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The design and development of covalent protein-protein interaction inhibitors for cancer treatment.
Journal of Hematology & Oncology ( IF 29.5 ) Pub Date : 2020-03-30 , DOI: 10.1186/s13045-020-00850-0
Sha-Sha Cheng 1 , Guan-Jun Yang 1 , Wanhe Wang 2, 3 , Chung-Hang Leung 1 , Dik-Lung Ma 2
Affiliation  

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.

中文翻译:

用于癌症治疗的共价蛋白-蛋白相互作用抑制剂的设计和开发。

蛋白质-蛋白质相互作用(PPI)是多种生物学过程的核心,其功能障碍与多种人类疾病(包括癌症)的发病机制有关。因此,抑制PPIs在药物开发中引起了极大的关注。据报道,共价抑制剂通过与靶蛋白中的半胱氨酸或其他亲核残基形成共价键来实现高效。有证据表明,降低了对共价药物耐药性的风险,这是在肿瘤学和传染病等领域的主要挑战。结构生物学和化学反应性的最新改进使得有效和选择性共价PPI抑制剂的设计和开发成为可能。在这篇评论中
更新日期:2020-04-22
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