Title:Recent Advances on PKM2 Inhibitors and Activators in Cancer
Applications
Volume: 31
Issue: 20
关键词:
PKM2,抑制剂,激活剂,抗肿瘤,生物医学应用,调节剂。
摘要: Metabolic reprogramming of cells, from the normal mode of glucose
metabolism named glycolysis, is a pivotal characteristic of impending cancerous cells.
Pyruvate kinase M2 (PKM2), an important enzyme that catalyzes the final rate-limiting
stage during glycolysis, is highly expressed in numerous types of tumors and aids in development
of favorable conditions for the survival of tumor cells. Increasing evidence
has suggested that PKM2 is one of promising targets for innovative drug discovery, especially
for the developments of antitumor therapeutics. Herein, we systematically summarize
the recent advancement on PKM2 modulators including inhibitors and activators
in cancer applications. We also discussed the classifications of pyruvate kinases in mammals
and the biological functions of PKM2 in this review. We do hope that this review
would provide a comprehensive understanding of the current research on PKM2 modulators,
which may benefit the development of more potent PKM2-related drug candidates
to treat PKM2-associated diseases including cancers in future.