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

NMR identification of anti-influenza lead compound targeting at PA_C subunit of H5N1 polymerase
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摘要 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,18β-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 PA_C as a target,and provided a starting point for the further discovery of new anti-influenza drugs. 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,18β-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 PA_C as a target,and provided a starting point for the further discovery of new anti-influenza drugs.
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2012年第1期89-92,共4页 中国化学快报(英文版)
基金 supported by the National Natural Science Foundation of China(No.81072576) to Y.L.Tang the National Natural Science Foundation of China(No. 30925011) the Ministry of Science and Technology 863 Project(No.2006AA02A314) to Y.F.Liu
关键词 PAC RNA polymerase inhibitor Anti-influenza agent Licorice-derived compounds PAC RNA polymerase inhibitor Anti-influenza agent Licorice-derived compounds
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