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.
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Authors | Li Cheng, Can-Rong Wu, Li-Han Zhu, Hua Li, Li-Xia Chen |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 27
Issue 5
Pg. 1243-1246
(03 01 2017)
ISSN: 1464-3405 [Electronic] England |
PMID | 28174105
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2017 Elsevier Ltd. All rights reserved. |
Chemical References |
- Antineoplastic Agents
- Ligands
- Withanolides
- physapubescin
- Glutaminase
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Topics |
- Animals
- Antineoplastic Agents
(chemistry, pharmacology)
- Biological Assay
- Cell Line, Tumor
- Enzyme Activation
(drug effects)
- Glutaminase
(antagonists & inhibitors)
- Humans
- Inhibitory Concentration 50
- Kidney
(enzymology)
- Ligands
- Molecular Docking Simulation
- Molecular Structure
- Solanaceae
(chemistry)
- Withanolides
(chemistry, pharmacology)
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