PROTACs:白血病治疗的未来

PROTACs: The Future of Leukemia Therapeutics.

作者信息

Anwar Zubair, Ali Muhammad Shahzad, Galvano Antonio, Perez Alessandro, La Mantia Maria, Bukhari Ihtisham, Swiatczak Bartlomiej

机构信息

Department of Surgical, Oncological, and Oral Sciences, Section of Medical Oncology, Uiniversity of Palermo, Palermo, Italy.

Department of Clinical and Biological Sciences, University of Turin, San Luigi Hospital, Turin, Italy.

出版信息

Front Cell Dev Biol. 2022 Sep 2;10:851087. doi: 10.3389/fcell.2022.851087. eCollection 2022.

Abstract

The fight to find effective, long-lasting treatments for cancer has led many researchers to consider protein degrading entities. Recent developments in PROteolysis TArgeting Chimeras (PROTACs) have signified their potential as possible cancer therapies. PROTACs are small molecule, protein degraders that function by hijacking the built-in Ubiquitin-Proteasome pathway. This review mainly focuses on the general design and functioning of PROTACs as well as current advancements in the development of PROTACs as anticancer therapies. Particular emphasis is given to PROTACs designed against various types of Leukemia/Blood malignancies.

摘要

寻找有效、持久的癌症治疗方法的努力促使许多研究人员考虑蛋白质降解实体。蛋白酶靶向嵌合体(PROTACs)的最新进展表明了它们作为潜在癌症治疗方法的可能性。PROTACs是小分子蛋白质降解剂,通过劫持内置的泛素-蛋白酶体途径发挥作用。本综述主要关注PROTACs的一般设计和功能,以及PROTACs作为抗癌疗法开发的当前进展。特别强调了针对各种类型白血病/血液恶性肿瘤设计的PROTACs。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe8d/9479449/148125368c8f/fcell-10-851087-g001.jpg

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