烟酰胺腺嘌呤二核苷酸(NAD)是生命体内200多种氧化还原反应的辅酶,在很多细胞生理过程中发挥着重要作用。烟酰胺磷酸核糖转移酶(Nampt)是哺乳动物NAD合成途径的限速酶,调节着细胞内的NAD水平,是生物体内进行各种生命活动和能量代谢的重要蛋白,具有多种生物学活性。在癌症中,肿瘤细胞为了快速增殖,对细胞内NAD水平的依赖比正常细胞更强。研究表明Nampt有促血管生成活性,支持着一些肿瘤细胞的生长,抑制Nampt酶活性可起到很好的抗肿瘤作用。这使得Nampt成为近年来药物研究中一个非常有吸引力的靶标,Nampt抑制剂被用于肿瘤化疗干预研究。目前有研究报道的Nampt抑制剂共4个:FK866、CHS828、CB30865、IS001。本文就近年来Nampt抑制剂在肿瘤治疗方面的研究进展进行综述,以期为Nampt调控剂的开发和应用提供参考。 Nicotinamide adenine dinucleotide (NAD) is the coenzyme of more than 200 kinds of redox reactions in vivo, and plays an important role in many cell physiological processes. Nicotinamide is a rate-limiting enzyme in mammalian NAD synthesis pathway and regulates intracellular NAD levels. It is an important protein in the body for various life activities and energy metabolism, and has a variety of biological activities. In cancer, tumor cells rely on NAD levels in cells more rapidly than normal cells for rapid proliferation. Studies have shown that Nampt pro-angiogenic activity, supporting the growth of some tumor cells, inhibition of Nampt enzyme activity can play a good anti-tumor effect. This makes Nampt a very attractive target for drug research in recent years, and Nampt inhibitors are used in cancer chemotherapeutic intervention studies. Currently there are four Nampt inhibitors reported in the study: FK866, CHS828, CB30865, IS001. This review summarizes the progress of Nampt inhibitors in the treatment of cancer in recent years, in order to provide a reference for the development and application of Nampt regulators.