p53基因位于17p13.1染色体,包含11个外显子及10个内含子区,编码的p53蛋白由N端转录激活结构域(Transactivation domain,TAD)、富含脯氨酸结构域(Proline-rich domain,PRD)、中央的DNA结合结构域(DNA-binding domain,DBD)、寡聚化结构域(Tetramerization domain,OD)和C末端调控域(C-Terminal domain,CTD)5大结构域组成...
Soln structure p53 core domainFersht, A R
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其他公司的靶向p53-MDM2相互作用的小分子也遭遇了挫折。诺华公司（Novartis）在1月份宣布停止用于急性髓系...
这为抗癌药物开发指明了一条新途径。 原始出处： Jing Zhao, Alan Blayney.et al.EGCG binds intrinsically disordered N-terminal domain of p53 and disrupts p53-MDM2 interaction.Nature Communications (2021). DOI: 10.1038/s41467-021-21258-5 原标题：《Nat Commun：绿茶竟可增强p53的抗癌活性？》
【2】Kussie, Paul H., et al. "Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain." Science 274.5289 (1996):948-953.doi:10.1126/science.274.5289.948 【3】Tyler, Andrew F. , et al. "Reactivation of the p53 tumor suppressor pathway by a stapled ...
: 225-239. e8.[10]. Lambert J M R,Gorzov P, Veprintsev D B, et al. PRIMA-1 reactivates mutant p53 by covalentbinding to the core domain[J]. Cancer cell, 2009, 15(5): 376-388.[11]. https://clinicaltrials.gov/ct2/show/NCT03745716?term=APR-246&phase=2&draw=2&rank=1 ...
Mis-sense mutations affecting TP53 promote carcinogenesis both by inactivating tumor suppression, and by conferring pro-carcinogenic activities. We report here that p53 DNA-binding domain (DBD) and transactivation domain (TAD) mis-sense mutants unexpecte
p53蛋白修饰的相关结构域:-反式激活结构域(transactivation domain):氨基酸1-42的N端部分构成。-富含脯氨酸结构域(proline-rich domain):从氨基酸63-97(各参考文献数值有些许出入),被证明是p53依赖的凋亡和细胞周期阻滞所必需的。-DNA结合结构域(DNA-binding domain,DBD): 富含精氨酸,与转录活性相关。-四聚化相关...
et al. A peptide that binds and stabilizes p53 core domain: chaperone strategy for rescue of oncogenic mutants. Proc. Natl Acad. Sci. USA 99, 937–942 (2002). Article CAS PubMed PubMed Central Google Scholar Issaeva, N. et al. Rescue of mutants of the tumor suppressor p53 in cancer...