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ID: ALA3994651

Journal: Bioorg Med Chem Lett

Title: Physapubescin, a natural withanolide as a kidney-type glutaminase (KGA) inhibitor.

Authors: Cheng L, Wu CR, Zhu LH, Li H, Chen LX.

Abstract: Kidney-type glutaminase (KGA) is over expressed in many kinds of cancers that converts glutamine to glutamate for supplying energy, and has become an object for targeted cancer therapy. The structure-based virtual ligand screening identified physapubescin, a withanolide purified from Physalis pubescens L., as a possible inhibitor of KGA with low binding energy. Enzyme inhibition experiments and cell-based assays further confirmed its inhibitory effects on KGA activity, suggesting potential applications of physapubescin and its derivatives as KGA inhibitors.

CiteXplore: 28174105

DOI: 10.1016/j.bmcl.2017.01.057