Clitocine是一种腺苷核苷类似物，是一种有效的通透剂(readthrough)。Clitocine可诱导携带p53无义突变等位基因的细胞产生p53蛋白。Clitocine可通过靶向Mcl-1诱导多药耐药肿瘤细胞凋亡。具有抗癌活性。
Clitocine, an adenosine nucleoside analog, is a potent and efficacious readthrough agent. Clitocine can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity[1][2].
Clitocine (0-0.8μM; 24 hours) enhances TRAIL-lethality in in LS411N and SW620 cells. Clitocine (0.2μM; 36 hours) significantly potentiates TRAIL-mediated apoptosis[2].
Citocine (0.3-3 mg/kg; s.c.; five times per week)-induced p53 inhibits CAOV-33p53-UAA136 tumor growth in a xenograft model[1]. Animal Model: nu/nu mice (CAOV-3p53-UAA136 xenograft tumors)[1]
[1]. Friesen WJ, et al. The nucleoside analog clitocine is a potent and efficacious readthrough agent. RNA. 2017;23(4):567-577. [2]. Sun JG, et al. Clitocine potentiates TRAIL-mediated apoptosis in human colon cancer cells by promoting Mcl-1 degradation. Apoptosis. 2016;21(10):1144-1157.
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