4.7 Article

NMR identification of anti-influenza lead compound targeting at PAC subunit of H5N1 polymerase

期刊

CHINESE CHEMICAL LETTERS
卷 23, 期 1, 页码 89-92

出版社

ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2011.09.006

关键词

PAC; RNA polymerase inhibitor; Anti-influenza agent; Licorice-derived compounds

资金

  1. National Natural Science Foundation of China [81072576, 30925011]
  2. Ministry of Science and Technology [2006AA02A314]

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PA(C) subunit from avian influenza (H5N1) viral RNA polymerase was used in this work as a target in the screening for anti-influenza agents from licorice-derived compounds. As a result, 18 beta-glycyrrhetinic acid was suggested to be PA(C) ligand by flexible docking, and was then confirmed by relaxation-edited NMR. The result of ApG primer extension assay indicated that this PA(C) ligand can inhibit the polymerase activity, and thus may potentially be valuable as anti-influenza lead compound. This work validated the possibility of screening polymerase inhibitors by using PAc as a target, and provided a starting point for the further discovery of new anti-influenza drugs. (C) 2011 Ya Lin Tang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

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