Back to Search
Start Over
Targeting cancer metabolism to develop human lactate dehydrogenase (hLDH)5 inhibitors.
- Source :
-
Drug discovery today [Drug Discov Today] 2018 Jul; Vol. 23 (7), pp. 1407-1415. Date of Electronic Publication: 2018 May 08. - Publication Year :
- 2018
-
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.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Antineoplastic Agents chemistry
Enzyme Inhibitors chemistry
Humans
Isoenzymes antagonists & inhibitors
Isoenzymes chemistry
Isoenzymes metabolism
L-Lactate Dehydrogenase chemistry
L-Lactate Dehydrogenase metabolism
Lactate Dehydrogenase 5
Models, Molecular
Neoplasms enzymology
Neoplasms pathology
Protein Conformation
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Drug Discovery methods
Energy Metabolism drug effects
Enzyme Inhibitors pharmacology
L-Lactate Dehydrogenase antagonists & inhibitors
Molecular Targeted Therapy
Neoplasms drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1878-5832
- Volume :
- 23
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Drug discovery today
- Publication Type :
- Academic Journal
- Accession number :
- 29750903
- Full Text :
- https://doi.org/10.1016/j.drudis.2018.05.014