PROTAC技术在药物研发领域具有广泛的应用前景。它可以用于开发针对各种疾病的新型药物,如癌症、神经退行性疾病、炎症性疾病等。通过特异性地降解与疾病相关的蛋白质,PROTAC技术可以实现精准治疗,提高治疗效果并降低副作用。此外,PROTAC技术还可以用于研究蛋白质的功能和调控机制,为生物学和医学研究提供有力的工具。 目前,...
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...
proteolysis targeting chimerastroketargeted degradationNeurological diseases such as stroke,Alzheimer's disease,Parkinson's disease,and Huntington's disease are among the intractable diseases for which appropriate drugs and treatments are lacking.Proteolysis targeting chimera(PROTAC)technology is a novel ...
作者: 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...
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。
Another challenge is the limited number of E3 ligases available for use in PROTAC design. While there are hundreds of E3 ligases in human cells, only a few are currently being utilized for therapeutic purposes. Expanding the repertoire of E3 ligases...
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 chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal degrada
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI). PROTACs are potentially superior to conventional small molecule inhibitors (SMIs) be
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