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PROTAC技术:机遇与挑战。

PROTAC Technology: Opportunities and Challenges.

作者信息

Gao Hongying, Sun Xiuyun, Rao Yu

机构信息

MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing 100084, P.R. China.

Tsinghua University-Peking University Joint Center for Life Sciences, Beijing 100084, P.R. China.

出版信息

ACS Med Chem Lett. 2020 Mar 12;11(3):237-240. doi: 10.1021/acsmedchemlett.9b00597.

Abstract

PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies. PROTACs opened a new chapter for novel drug development. However, any new technology will face many new problems and challenges. Perspectives on the potential opportunities and challenges of PROTACs will contribute to the research and development of new protein degradation drugs and degrader tools.

摘要

PROTAC诱导的靶向蛋白降解已成为药物开发中的一种新型治疗策略,并受到学术机构、大型制药企业(如阿斯利康、拜耳、诺华、安进、辉瑞、葛兰素史克、默克和勃林格殷格翰等)以及生物技术公司的青睐。PROTAC为新型药物开发开启了新篇章。然而,任何新技术都会面临许多新问题和挑战。对PROTAC潜在机遇和挑战的展望将有助于新型蛋白降解药物和降解剂工具的研发。

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PROTAC Technology: Opportunities and Challenges.PROTAC技术:机遇与挑战。
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本文引用的文献

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Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.作为一种治疗方式的 Cereblon 介导的蛋白质降解的演变
ACS Med Chem Lett. 2019 Nov 12;10(12):1592-1602. doi: 10.1021/acsmedchemlett.9b00425. eCollection 2019 Dec 12.
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Targeting IRAK4 for Degradation with PROTACs.利用PROTAC技术靶向降解白细胞介素-1受体相关激酶4(IRAK4)
ACS Med Chem Lett. 2019 Jun 14;10(7):1081-1085. doi: 10.1021/acsmedchemlett.9b00219. eCollection 2019 Jul 11.

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