期刊
SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY
卷 132, 期 -, 页码 213-229出版社
ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD
DOI: 10.1016/j.semcdb.2022.02.007
关键词
Ubiquitin ligase; Deubiquitinase; Cancer; Structure -based drug design; Preclinical screening; Clinical trial
资金
- European Regional Development Fund (ERDF) through the Interreg V-A Spain-France-Andorra (POCTEFA) program, project PROTEOblood [EFA360/19]
- Fondo de Investigacion Sanitaria [PI18/01383]
This review provides an update on the major scientific breakthroughs in ubiquitin-targeting therapies in the past decade, with a focus on E1 and E3 modulators. It also discusses the unique challenges of identifying new potential therapeutic targets within this complex system and explores chemical approaches to meet these challenges.
As a post-translational modification that has pivotal roles in protein degradation, ubiquitination ensures that intracellular proteins act in a precise spatial and temporal manner to regulate diversified cellular processes. Perturbation of the ubiquitin system contributes directly to the onset and progression of a wide variety of diseases, including various subtypes of cancer. This highly regulated system has been for years an active research area for drug discovery that is exemplified by several approved drugs. In this review, we will provide an update of the main breakthrough scientific discoveries that have been leading the clinical development of ubiquitintargeting therapies in the last decade, with a special focus on E1 and E3 modulators. We will further discuss the unique challenges of identifying new potential therapeutic targets within this ubiquitous and highly complex machinery, based on available crystallographic structures, and explore chemical approaches by which these challenges might be met.
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