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Updated: Feb 10, 2026

Mapping Metabolism: Monitoring Lactate Dehydrogenase Activity Directly in Tissue
Published on: June 21, 2018
Targeting cancer metabolism to develop human lactate dehydrogenase (hLDH)5 inhibitors
Shao-Lin Zhang1, Yun He1, Kin Yip Tam2
1Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, 55 Daxuecheng South Road, Shapingba, Chongqing 401331, PR China.
Abstract:
Cancer cells feature a switch in glucose metabolism from oxidative phosphorylation to cytoplasm-based glycolysis. This altered cellular metabolic pathway meets the survival and proliferation needs for tumor progression. Targeting the metabolic remodeling could offer opportunities for developing effective anticancer therapeutics. Human lactate dehydrogenase (hLDH)5 plays a crucial part in the promotion of glycolysis and is overexpressed in various human tumors, and thus could be a potential anticancer drug target. Here, we briefly discuss the roles of hLDH5 and its connections with cancer metabolism. Then, we review the reported small molecules in light of their binding modes to hLDH5. Finally, possible directions for future development of hLDH5 inhibitors are proposed. We hope that this review will provoke interest in developing hLDH5 inhibitors.
Insights
Cancer cells rely on glycolysis, a metabolic pathway promoted by human lactate dehydrogenase (hLDH)5. Inhibiting hLDH5 offers a promising strategy for developing novel anticancer therapeutics targeting tumor metabolism.
Area of Science:
- Biochemistry
- Oncology
- Metabolic pathways
Background:
- Cancer cells exhibit altered glucose metabolism, shifting from oxidative phosphorylation to glycolysis.
- This metabolic reprogramming supports tumor survival and proliferation.
- Human lactate dehydrogenase (hLDH)5 is overexpressed in tumors and promotes glycolysis.
Purpose of the Study:
- To review the role of hLDH5 in cancer metabolism.
- To discuss small molecules targeting hLDH5 based on their binding modes.
- To propose future directions for hLDH5 inhibitor development.
Main Methods:
- Literature review of hLDH5's role in cancer.
- Analysis of small molecule inhibitors and their binding interactions with hLDH5.
- Exploration of potential therapeutic strategies.
Main Results:
- hLDH5 is a key enzyme in cancer glycolysis.
- Various small molecules targeting hLDH5 have been reported.
- Understanding binding modes is crucial for inhibitor design.
Conclusions:
- Targeting hLDH5 represents a viable strategy for anticancer drug development.
- Further research into hLDH5 inhibitors could lead to effective cancer therapeutics.
- hLDH5 is a significant target for modulating cancer metabolism.
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