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p53 reactivation: The link to zinc

机译:p53激活:与锌的联系

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摘要

Lack of p53 expression or expression of mutant p53 is common in human cancers and is associated with increased tumor growth and resistance to therapies. Significant efforts toward pharmaceutical reactivation of defective p53 by small molecules are therefore underway, targeting the different means that inactivate p53. Indeed, reactivated p53 can lead to tumor destruction. A recent paper in Cancer Cell by Yu et al. describes reactivation of mutant p53 (mtp53) by thiosemicarbazone compounds.5 These compounds induce wild-type (wt)p53 conformation, in particular for the p53H175 mutant, and this restores p53-dependent apoptosis and inhibition of xenograft tumor growth.
机译:缺乏p53表达或突变体p53的表达在人类癌症中很常见,并且与肿瘤生长和对治疗的抗性增加有关。因此,正在努力通过小分子对有缺陷的p53进行药物再活化,以使p53失活的不同方法为目标。实际上,重新激活的p53可导致肿瘤破坏。 Yu等人最近在《癌细胞》上发表的论文。 5描述了这些化合物诱导野生型(wt)p53构象,特别是对于p53H175突变体,并恢复了p53依赖性细胞凋亡并抑制了异种移植肿瘤的生长。

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