%0 Journal Article
%T 靶向激酶的PROTAC研究进展<br>Progress in the Research of Kinases PROTAC
%A 陈泉威
%A 王昭昭
%A 朱雍
%A 陆涛
%J Hans Journal of Medicinal Chemistry
%P 9-20
%@ 2331-8295
%D 2022
%I Hans Publishing
%R 10.12677/HJMCe.2022.101002
%X 蛋白激酶(PK)失调与多种疾病过程相关，多种蛋白激酶抑制剂得被开发用以治疗疾病。蛋白激酶抑制剂虽然得到了很好的研究，但仍然面临耐药性及选择性不高等挑战。蛋白水解靶向嵌合体(PROTAC)这一技术的开发，有效地解决了蛋白激酶抑制剂耐药以及低选择性等问题，从而得到了广泛的关注。目前，已经有多种激酶PROTAC项目进入临床前和临床研究。本文综述了专利及文献报道的靶向蛋白激酶的PROTAC研究进展。总结并展望靶向蛋白质降解技术的发展前景，及面临的机遇与挑战。<br />
Protein kinase (PK) disorders are associated with a variety of disease processes, and multiple pro-tein kinase inhibitors have been developed to treat disease. Although protein kinase inhibitors are well developed, there still are challenges of drug resistance and low selectivity. The development of proteolytic targeted chimera (PROTAC) technology has effectively solved the drug resistance of the protein kinase inhibitor and side effects caused by low selectivity, which has received widespread attention. Currently, a variety of kinase PROTAC projects have entered preclinical and clinical stud-ies. This article reviews the research progress of patented and literature-reported PROTAC target-ing protein kinases. Summarize and look forward to the development prospects of targeted protein degradation technology, as well as the opportunities and challenges.
%K 蛋白激酶，蛋白水解嵌合体，耐药，选择性<br>Protein Kinases
%K Proteolysis Targeting Chimera
%K Drug Resistance
%K Selectivity
%U http://www.hanspub.org/journal/PaperInformation.aspx?PaperID=48164