Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 5, Pages 1243-1246Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.01.057
Keywords
Physapubescin; KGA inhibitor; Structure-based virtual ligand screening; Enzyme inhibition; Cytotoxicity
Categories
Funding
- National Natural Science Foundation of China (NSFC) [31270399]
- Liaoning Province Natural Science Foundation [201602689]
- Scientific Research Foundation for the Returned Overseas Chinese Scholars of Shenyang Pharmaceutical University [GGJJ2015103]
- Career Development Program for Young and Middle-aged Teachers of Shenyang Pharmaceutical University [ZQN2015015]
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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. (C) 2017 Elsevier Ltd. All rights reserved.
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