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Issue 3, 2017
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Discovery of potent human lactate dehydrogenase A (LDHA) inhibitors with antiproliferative activity against lung cancer cells: virtual screening and biological evaluation

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Abstract

Human lactate dehydrogenase A (LDHA) plays a crucial role in the promotion of glycolysis in invasive tumor cells, and recently, it has been considered as a vital therapeutic target in the field of oncology. Herein, by combining docking-based virtual screening with in vitro biochemical evaluation, we report the discovery of a potent LDHA inhibitor with antiproliferative activity. The enzymatic assay suggested that the identified compound 7 has a good inhibitory activity (IC50 = 0.36 μM) against LDHA. The in vitro cytotoxicity assay demonstrated that compound 7 reduces the growth of A549 and NCI-H1975 lung cancer cells, with EC50 values of 5.5 and 3.0 μM, respectively. These findings indicate that compound 7 could be employed as a useful probe to explore the pharmacology of LDHA.

Graphical abstract: Discovery of potent human lactate dehydrogenase A (LDHA) inhibitors with antiproliferative activity against lung cancer cells: virtual screening and biological evaluation

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Publication details

The article was received on 01 Dec 2016, accepted on 10 Jan 2017, published on 13 Jan 2017 and first published online on 13 Jan 2017


Article type: Research Article
DOI: 10.1039/C6MD00670A
Citation: Med. Chem. Commun., 2017,8, 599-605
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    Discovery of potent human lactate dehydrogenase A (LDHA) inhibitors with antiproliferative activity against lung cancer cells: virtual screening and biological evaluation

    X. Li, W. Xiao and H. Zhao, Med. Chem. Commun., 2017, 8, 599
    DOI: 10.1039/C6MD00670A

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