2. Academic Validation
  3. A novel inhibitor of PGK1 suppresses the aerobic glycolysis and proliferation of hepatocellular carcinoma

A novel inhibitor of PGK1 suppresses the aerobic glycolysis and proliferation of hepatocellular carcinoma

  • Biomed Pharmacother. 2023 Feb:158:114115. doi: 10.1016/j.biopha.2022.114115.
Mingfeng Li 1,  Aotong Zhang 1,  Xin Qi 1,  Rilei Yu 1,  Jing Li 2
Affiliations

Affiliations

  • 1 Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People's Republic of China.
  • 2 Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People's Republic of China; Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology, 266237, People's Republic of China. Electronic address: lijing_ouc@ouc.edu.cn.
PMID: 36516697 DOI: 10.1016/j.biopha.2022.114115
Abstract

Phosphoglycerate kinase 1(PGK1) is an important enzyme in the metabolic glycolysis pathway. Nowadays, PGK1 is an appealing therapeutic target for multiple cancers. However, no effective inhibitor of PGK1 has been reported. In this study, we demonstrate that Ilicicolin H a 5-(4-hydroxyphenyl)-pyridone with a decalin ring system and a non-ATP-competitive inhibitor of PGK1, inhibits the proliferation and promotes Apoptosis of Hepatocellular carcinoma (HCC). Many Cancer cells display enhanced glycolysis which is critical for tumor development. Here we identified that Ilicicolin H can target PGK1 in vitro to inhibit the lactate production and glucose uptake of HCC cells. These findings suggest that the PGK1 inhibitor- Ilicicolin H is a promising Anticancer agent and may provide a better therapeutic strategy for HCC treatment in the future.

Keywords

Anti-cancer; Hepatocellular carcinoma; Inhibitor; PGK1.

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