尼克酰胺磷酸核糖转移酶抑制剂的抗肿瘤作用研究进展

Advances of Anti-tumor Effects of Nicotinamide Phosphoribosyltransferase Inhibitors

关键词:  尼克酰胺磷酸核糖转移酶  尼克酰胺腺嘌呤二核苷酸  肿瘤  NAMPT抑制剂

Key words:  nicotinamide phosphoribosyltransferase  nicotinamide adenine dinucleotide  tumor  NAMPT inhibitor

摘要:

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。

Abstract:

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.