Small-molecule inhibitors of human LDH5
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Carlotta Granchi1, Ilaria Paterni, Reshma Rani
1Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Abstract:
The latest findings on the role played by human LDH5 (hLDH5) in the promotion of glycolysis in invasive tumor cells indicates that this enzyme subtype is a promising therapeutic target for invasive cancer. Compounds able to selectively inhibit hLDH5 hold promise for the cure of neoplastic diseases. hLDH5 has so far been a rather unexplored target, since its importance in the promotion of cancer progression has been neglected for decades. This enzyme should also be considered as a challenging target due the high polar character (mostly cationic) of its ligand cavity. Recently, significant progresses have been reached with small-molecule inhibitors of hLDH5 displaying remarkable potencies and selectivities. This review provides an overview of the newly developed hLDH5 inhibitors. The roles of hLDH isoforms will be briefly discussed, and then the inhibitors will be grouped into chemical classes. Furthermore, general pharmacophore features will be emphasized throughout the structural subgroups analyzed.
Insights
Human LDH5 (hLDH5) is a key enzyme in invasive cancer glycolysis and a promising therapeutic target. Recent small-molecule inhibitors show high potency and selectivity, offering hope for treating neoplastic diseases.
Area of Science:
- Biochemistry
- Oncology
- Medicinal Chemistry
Background:
- Human lactate dehydrogenase 5 (hLDH5) promotes glycolysis in invasive tumor cells.
- hLDH5 has been historically underexplored as a cancer therapeutic target.
- The enzyme's cationic ligand cavity presents a challenge for inhibitor development.
Purpose of the Study:
- To review recent advancements in small-molecule inhibitors targeting hLDH5.
- To discuss the role of hLDH isoforms in cancer progression.
- To analyze the pharmacophore features of novel hLDH5 inhibitors.
Main Methods:
- Literature review of recent findings on hLDH5 inhibitors.
- Classification of inhibitors based on chemical classes.
- Analysis of pharmacophore characteristics within structural subgroups.
Main Results:
- Significant progress has been made in developing potent and selective small-molecule hLDH5 inhibitors.
- Newly developed inhibitors demonstrate promise for cancer therapy.
- Pharmacophore analysis provides insights into inhibitor design.
Conclusions:
- hLDH5 is a viable and promising therapeutic target for invasive cancers.
- Selective hLDH5 inhibition offers a potential strategy for treating neoplastic diseases.
- Ongoing research is yielding effective inhibitors with desirable properties.
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