2. Academic Validation
  3. Targeting PGAM1 in cancer: An emerging therapeutic opportunity

Targeting PGAM1 in cancer: An emerging therapeutic opportunity

  • Eur J Med Chem. 2022 Dec 15:244:114798. doi: 10.1016/j.ejmech.2022.114798.
Guan-Jun Yang 1,  Fan Tao 2,  Hai-Jing Zhong 3,  Chao Yang 4,  Jiong Chen 5
Affiliations

Affiliations

  • 1 State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, 315211, Zhejiang, China; Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, 315211, China; Key Laboratory of Aquacultural Biotechnology Ministry of Education, Ningbo University, Ningbo, 315211, China.
  • 2 State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, 315211, Zhejiang, China.
  • 3 Institute of New Drug Research and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy, Guangzhou, 510632, China. Electronic address: zhonghaijing88@gmail.com.
  • 4 National Engineering Research Center for Marine Aquaculture, Institute of Innovation & Application, Zhejiang Ocean University, Zhoushan, Zhejiang Province, 316022, China. Electronic address: yc52028@hotmail.com.
  • 5 State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, 315211, Zhejiang, China; Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, 315211, China; Key Laboratory of Aquacultural Biotechnology Ministry of Education, Ningbo University, Ningbo, 315211, China. Electronic address: chenjiong@nbu.edu.cn.
PMID: 36215859 DOI: 10.1016/j.ejmech.2022.114798
Abstract

Glycolysis is a preferred metabolic pattern of Cancer cells. Phosphoglycerate mutase 1 (PGAM1) is a pivotal glycolytic Enzyme that catalyzes the reciprocal conversion between 2-phosphoglycerate and 3-phosphoglycerate. It also stimulates anabolic pathways, generates adenosine triphosphate, and keeps redox balance under hypoxic conditions. Mounting evidence supports that PGAM1 is overexpressed in many cancers and promotes their progression. The critical roles of PGAM1 in tumorigenesis make it a promising theranostical target for Cancer. The aberrant expression of PGAM1 enables it to become a potential diagnosis gene for several cancers, and its heterogeneous regulations via interacting with its different ligands increase the possibility of it as a target for Cancer therapy and discovery of tens of PGAM1 inhibitors, which can provide the potential feasibility for Cancer treatment. This review provides insights into structure, function, and regulation of PGAM1, summarizes its mechanism in tumorigenesis, reviews the advanced status of PGAM1 inhibitors in Cancer diagnosis and treatment, and finally emphasizes PGAM1 as an appealing theranostical target for Cancer.

Keywords

Cancer therapy; Glycolysis; Phosphoglycerate mutase 1; Structure-activity relationship.

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