尼克酰胺磷酸核糖转移酶抑制剂的抗肿瘤作用研究进展

尼克酰胺磷酸核糖转移酶(nicotinamide phosphoribosyltransferase,NAMPT)是哺乳动物细胞烟酰胺腺嘌呤二核苷酸(nicotinamide adenine dinucleotide,NAD)补救合成通路的限速酶。NAMPT通过合成NAD,参与调节细胞内重要的生理病理过程。近年研究发现,NAMPT与肿瘤发生、发展有着密切关系,抑制NAMPT可以起到有效的抗肿瘤作用。NAMPT已成为抗肿瘤药物研究新靶点,其抑制剂FK866、GMX1778作为抗肿瘤药,已经进入临床试验。NAMPT抑制剂作用机制的研究主要包括诱导细胞凋亡、细胞自吞噬、抑制细胞增殖、血管生成等。本文综述了NAMPT抑制剂的抗肿瘤作用及机制研究。

Advances of Anti-tumor Effects of Nicotinamide Phosphoribosyltransferase Inhibitors

Nicotinamide phosphoribosyltransferase(NAMPT) is the key enzyme in the salvaging biosynthetic pathway of nicotinamide adenine dinucleotide(NAD) in mammals cells. By synthesizing NAD, NAMPT is involved in many important cellular processes. In recent years, studies have shown that NAMPT is closely related with the occurrence and development of tumors, and the inhibition of NAMPT achieved anti-tumor effects. NAMPT has been recognized as a novel potential target of the treatment of tumors. NAMPT inhibitors including FK866 and GMX1778 have been registered for clinical trials on the treatment of tumors. NAMPT inhibitors can induce cell apoptosis, autophagy, and inhibit proliferation and angiogenesis. It is reviewed the recent advances of the studies on anti-tumor effects of NAMPT inhibitors.