以M2型丙酮酸激酶为靶点的抗肿瘤药物研究进展

Advances in antitumor drugs targeting pyruvate kinase M2

目前,肿瘤高发病率、高病死率以及难治愈性使其成为科学研究领域无法突破的难点。随着分子生物学的发展,针对肿瘤细胞特征而挖掘的分子靶点受到研究者的关注。M2型丙酮酸激酶(PKM2)是肿瘤细胞有氧糖酵解过程中的关键催化酶,其对糖酵解具有双重调控作用。因此,PKM2的抑制剂和激活剂均具有成为抗肿瘤候选药物的潜能。本文将对这一看似相悖的现象加以探讨,重点以PKM2为研究对象,介绍其在肿瘤发生发展中的双重作用,并对相关靶向药物加以阐述,为同类相关靶点的挖掘和抗肿瘤候选药物的研发提供理论依据。

At present,the high incidence,high lethality and refractoriness of the tumor still make it a great challenge for scientific research.With the development of molecular biology,molecular targets mined for tumor cell characteristics have received attention from researchers.Pyruvate kinase M2(PKM2)is a key catalytic enzyme in the aerobic glycolysis of tumor cells and has a dual role in regulating glycolysis.Therefore,both inhibitors and activators of PKM2 may be served as antitumor drug candidates.This paper is intended to discuss this seemingly contradictory speculation by focusing on PKM2 and introducing its dual role in tumor development,as well as describing the relevant target drugs,to provide a theoretical basis for the exploration of similar relevant targets and the research and development of anti-tumor drug candidates.