compound introduction
它是p73的突变体p53依赖性激活剂，p53调控基因的激活剂和携带突变体p53的肿瘤细胞的抑制剂。大于50％的肿瘤表达突变体p53，该突变体的肿瘤抑制功能存在缺陷，并通过阻断p53家族成员p73促成恶性肿瘤。在人类癌症中p73的激活产生细胞毒性作用。RETRA可提高p73的表达水平，并从具有突变体53的抑制复合物中释放p73。然后在体内和体外产生抑癌作用。 This is a mutant p53-dependent activator of p73, an activator of p53-regulated genes, and a suppressor of mutant p53-bearing tumor cells. Greater than 50% of tumors express mutant p53 which is defective for the tumor-suppressor function and contributes to malignancy by blocking a p53 family member p73. Activation of p73 in human cancer produces a cytotoxic effect. RETRA increases the expression level of p73 and releases p73 from the inhibitory complex with mutant 53. This then produces a tumor-supressor effect, in vitro and in vivo.
