PRIMA-1

p53肿瘤抑制因子的突变存在于许多不同的肿瘤细胞中。PRIMA-1在相对较高的µM至mM浓度下恢复突变p53蛋白的序列特异性DNA结合和转录激活活性。因此，它是一种独特的抗癌物质，通过功能特异性表位的构象调节，作为突变p53凋亡功能的再激活剂。PRIMA-1是一种新型先导化合物，可以进一步修饰以提供通过再激活机制起作用的更有效的治疗剂。Mutations in the p53 tumor suppressor are found in many different neoplastic cells. PRIMA-1 restores sequence-specific DNA binding and transactivational activity to mutant p53 proteins at relatively high µM to mM concentrations. It is therefore a unique anti-oncogenic substance, working as a re-activator of the apoptotic function of mutant p53 via conformational modulation of function-specific epitopes. PRIMA-1 represents a novel lead compound which may be further modified to provide more potent therapeutic agents acting via the reactivation mechanism.分子式C9H15NO3分子量185.2OCC1(CO)N2CCC(CC2)C1=O