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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。
Nicotinamide phosphoribosyltransferase (NAMPT) is a rate-limiting enzyme in the salvage-synthesis pathway of mammalian cells, nicotinamide adenine dinucleotide (NAD). NAMPT is involved in the regulation of important physiological and pathological processes in the cell through the synthesis of NAD. Recent studies have found that, NAMPT and tumor occurrence and development are closely related to inhibition of NAMPT can play an effective antitumor effect. NAMPT has become a new target for anticancer drug research, and its inhibitors FK866, GMX1778 as antineoplastic agents, have entered clinical trials. NAMPT inhibitor mechanism of action mainly includes the induction of apoptosis, cell autophagy, inhibition of cell proliferation, angiogenesis and so on. This article reviews the anti-tumor effect and mechanism of NAMPT inhibitors.