Identification of a potent inhibitor targeting human lactate dehydrogenase A and its metabolic modulation for cancer cell line.
Basic Information
ID: ALA3745616
Journal: Bioorg Med Chem Lett
Title: Identification of a potent inhibitor targeting human lactate dehydrogenase A and its metabolic modulation for cancer cell line.
Authors: Chen CY, Feng Y, Chen JY, Deng H.
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=0.25μM) to LDHA. Cytotoxic assay suggested that the VS-2 could inhibit MCF-7 cancer cell growth, with the IC50 value low to 1.54μM. 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.
CiteXplore: 26597536
DOI: 10.1016/j.bmcl.2015.11.025
Patent ID: ┄