PROTAC(Proteolysis Targeting Chimera)技术,即蛋白降解靶向嵌合体技术,是一种全新的药物研发策略。该技术通过利用细胞内天然的蛋白降解体系——泛素蛋白酶体系统(UPS),实现对目标蛋白(POI,protein of interest)的特异性降解。 PROTAC分子由三个主要部分组成:靶蛋白配体、连接子(Linker)和E3连接酶配体。靶蛋白配体能够...
靶向蛋白降解技术PROTAC(proteolysis-targeting chimera)突破“不可成药”问题,是全新的治疗平台。在传统的小分子抑制剂开发过程中,很多关键疾病靶点因为构象原因导致“不可成药”。PROTAC的本质是一个双功能小分子,一方面靶向目标蛋白,一方面招募泛素连接酶『O突破蛋白质“不可成药”的技术平台:靶向蛋白降...』O突破蛋...
每日一学:蛋白质水解靶向嵌合体(Proteolysis Targeting Chimera, PROTAC)技术应运而生。PROTAC就是靶向蛋白降解的小分子联合体,联合体分子包括三部分:一头是靶向目标蛋白的结构;另一头是可以招募蛋白降解体系比如E3连接酶的结构;中间则通过合适的连接器(linker)连接!蛋白降解疗法形象的比喻为给癌基因添加了叛军的标签,...
转发:PROTAC(Proteolysis-targeting chimera)全称蛋白降解靶向嵌合体,即利用泛素-蛋白酶体系统诱导靶向蛋白降解。与传统小分子药物不同,PROTAC无需与目标蛋白长时间和高强度的结合,便可捕获蛋白并将其降解,因此有望突破传统难以成药的靶点并克服耐药性问题。 PROTAC作为一项全新的小分子药物技术,可作用于传统靶向药物无...
This tutorial review discusses the convergence of drug delivery systems and PROTACs, surveys the burgeoning PROTAC delivery strategies, summarizes their design principles, clarifies their challenges, and outlooks future translational opportunities. Abstract Proteolysis Targeting Chimeras (PROTACs), an emergi...
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently linked ligand of an E3 ubiquitin ligase (E3...
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently linked ligand of an E3 ubiquitin ligase (E3...
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently linked ligand of an E3 ubiquitin ligase (E3...
靶向FAK的蛋白水解靶向嵌合体(proteolysis-targeting chimera,PROTAC)分子利用细胞内的泛素蛋白酶体系统实现对目标蛋白FAK的降解,能够同时影响FAK的激酶活性和支架蛋白... 许明诗 - 《华东师范大学》 被引量: 0发表: 2024年 PROteolysis‐Targeting Chimeras (PROTACs) in leukemia: overview and future perspectives PR...
靶向蛋白降解(TPD)技术的进展是药物发现领域的关键性转变,尤其是通过分子胶和蛋白降解靶向嵌合体(Proteolysis-Targeting Chimera,以下简称PROTAC),大大扩展了可成药的靶点,为治疗开辟了前所未有的可能性。当下,靶向蛋白降解领域正在蓬勃发展,新兴的技术和药物类型不断涌现。