Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368792 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
Targeting LDHA represents a promising strategy for the development of new anti-cancer agents. We report herein the identification of a potent compound as a direct LDHA inhibitor. The in vitro enzymatic assay revealed that the VS-2 had good inhibitory potency (IC50 = 0.25 μM) to LDHA. Cytotoxic assay suggested that the VS-2 could inhibit MCF-7 cancer cell growth, with the IC50 value low to 1.54 μM. The seahorse XF24 experiment validated that the VS-2 served as a modulator to reprogram MCF-7 cancer cell metabolism from glycolysis to mitochondrial respiration.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chun-Ye Chen, Yan Feng, Jing-Yu Chen, Hao Deng,