摘要
PROTAC (靶向嵌合体蛋白水解)技术是一种基于泛素-蛋白酶体系统的靶向蛋白降解策略,近年来逐渐发展成为一种潜在的靶向肿瘤治疗手段。该策略在药效学、选择性和耐药方面已经显示出比传统小分子抑制剂的显著优势。一些小分子PROTACs已进入I期临床试验。本文介绍了PROTACs策略的原理、特点和优势。并对小分子PROTACs在肿瘤治疗中的研究进展进行了综述。我们希望这篇综述将有助于优化理想的小分子PROTACs的设计,推进靶向抗癌研究。
关键词: 抗癌,E3连接酶,PROTAC,蛋白降解,泛素化,配体,转导。
Current Medicinal Chemistry
Title:Recent Advances in Small Molecule PROTACs for the Treatment of Cancer
Volume: 28 Issue: 24
关键词: 抗癌,E3连接酶,PROTAC,蛋白降解,泛素化,配体,转导。
摘要: The PROTAC (PROteolysis TArgeting Chimera) technology is a target protein degradation strategy, based on the ubiquitin-proteasome system, which has been gradually developed into a potential means of targeted cancer therapy in recent years. This strategy has already shown significant advantages over traditional small-molecule inhibitors in terms of pharmacodynamics, selectivity, and drug resistance. Several small molecule PROTACs have been in Phase I clinical trial. Herein, we have introduced the mechanism, characteristics, and advantages of PROTAC strategy. And we have summarized the recent advances in the development of small-molecule PROTACs for cancer treatment. We hope this review will be helpful in optimizing the design of the ideal small- molecule PROTACs and advancing targeted anticancer research.
Export Options
About this article
Cite this article as:
Recent Advances in Small Molecule PROTACs for the Treatment of Cancer, Current Medicinal Chemistry 2021; 28 (24) . https://dx.doi.org/10.2174/0929867327666201117141611
DOI https://dx.doi.org/10.2174/0929867327666201117141611 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
![](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements