PROTAC药物在前列腺癌治疗中的研究进展  

Research progress of PROTACs in the treatment of prostate cancer

作　　者：张思汗 夏启东 王少刚[1] Zhang Sihan;Xia Qidong;Wang Shaogang(Department of Urology,Tongji Hospital,Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,China)

机构地区：[1]华中科技大学同济医学院附属同济医院泌尿外科,武汉430030

出　　处：《中华泌尿外科杂志》2023年第11期873-876,共4页Chinese Journal of Urology

摘　　要：雄激素剥夺治疗无效或耐药、免疫治疗反应率低和小分子靶向药物疗效欠佳是目前前列腺癌药物治疗面临的主要难题。蛋白降解靶向嵌合体(PROTAC)通过将靶蛋白与泛素蛋白酶体系统连接,引发靶蛋白降解,在肿瘤治疗领域颇具发展潜力。近年来,以雄激素受体、细胞增殖及转录调控相关蛋白为靶点治疗前列腺癌的PROTAC药物的基础研究取得显著成果。PROTAC药物治疗前列腺癌的临床试验也正逐步开展。在精准治疗时代,PROTAC药物是前列腺癌药物治疗领域的全新突破。本文总结PROTAC药物的基本原理及其在前列腺癌治疗领域的研究进展。The major challenges in drug therapy for prostate cancer are the ineffectiveness and resistance to androgen deprivation therapy,the low response to immunotherapy and the poor efficacy of small molecule targeted drugs.As a brand-new drug design concept,proteolysis targeting chimera(PROTAC)reveals its strength in the field of cancer treatment by connecting the target protein to the ubiquitinproteasome system and triggering the degradation of the target protein.In recent years,basic medical research on targeting androgen receptors,cell proliferation,and transcriptional regulation proteins for the treatment of prostate cancer has achieved significant progress.Meanwhile,clinical trials related to PROTAC for the treatment of prostate cancer are gradually being carried out.In an era of big data and precision medicine,PROTAC is a breakthrough in the field of prostate cancer drug therapy.This article summarizes the fundamental principles of PROTACs and the basic and clinical research advances in the field of prostate cancer treatment.

关 键 词：前列腺肿瘤 癌 蛋白降解靶向嵌合体技术 治疗靶点 临床试验 

分 类 号：R737.25[医药卫生—肿瘤]