CD 437

CD 437是一种RARγ的选择性激动剂[1].

视黄酸受体γ(RAR-γ)是一种由9-顺式视黄酸和全反式视黄酸激活的核受体.RAR-γ还有作为转录因子的功能.

CD 437是一种选择性的RARγ激动剂.在肿瘤细胞中,CD437诱发RAR-γ依赖性的分化和细胞凋亡.另外,CD437诱发DNA加合物形成和p53非依赖性的DNA损伤反应[1].在DU145人前列腺癌细胞中,CD437快速减少IκBα,且增加NF-κB p65亚基的核易位.另外,CD437增强NF-κB 的DNA结合活性,且诱发DR4表达和细胞凋亡[2].在人黑色素瘤A375细胞中,CD437诱发由NF-κB和RIG-I(视黄酸诱导基因Ⅰ)信号通路活化介导的细胞凋亡[3].在人骨肉瘤细胞中,CD437通过上调硫氧还蛋白结合蛋白2(TBP2),激活c-Jun N端激酶1(JNK1),且诱发细胞凋亡.此外,CD437通过募集ETS1转录因子,诱发TBP2 mRNA的表达[4].

参考文献：
[1].  Zhao X, Spanjaard RA. The apoptotic action of the retinoid CD437/AHPN: diverse effects, common basis. J Biomed Sci, 2003, 10(1): 44-49.
[2].  Jin F, Liu X, Zhou Z, et al. Activation of nuclear factor-kappaB contributes to induction of death receptors and apoptosis by the synthetic retinoid CD437 in DU145 human prostate cancer cells. Cancer Res, 2005, 65(14): 6354-6363.
[3].  Pan M, Geng S, Xiao S, et al. Apoptosis induced by synthetic retinoic acid CD437 on human melanoma A375 cells involves RIG-I pathway. Arch Dermatol Res, 2009, 301(1): 15-20.
[4].  Hashiguchi K, Tsuchiya H, Tomita A, et al. Involvement of ETS1 in thioredoxin-binding protein 2 transcription induced by a synthetic retinoid CD437 in human osteosarcoma cells. Biochem Biophys Res Commun, 2010, 391(1): 621-626.