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基于流感病毒PAN蛋白的高通量药物筛选

, PP. 181-186

Keywords: 流感病毒,PAN蛋白,高通量药物筛选,分子对接,化合物

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Abstract:

流感病毒的PAN蛋白高度保守,并且具有核酸内切酶活性,是抗流感药物研发的潜在靶点。通过高通量药物筛选体系,从372种化合物中筛选出3种对流感病毒H5N1的PAN蛋白抑制作用较好的化合物。将这3种化合物分别与PAN蛋白进行分子对接模拟,结果显示它们均可以与PAN蛋白活性位点的二价金属离子和氨基酸残基相互作用,从而为抗流感病毒药物的发现提供了先导化合物。

References

[1]  Webby RJ, Swenson SL, Krauss SL, et al. Evolution of swine H3N2 influenza viruses in the United States[J]. Journal of Virology, 2000, 74(18):8243-8251. [2] Karasin AI, Schutten MM, Cooper LA, et al. Genetic characterization of H3N2 influenza viruses isolated from pigs in North America, 1977-1999:evidence for wholly human and reassortant virus genotypes[J]. Virus Research, 2000, 68(1):71-85. [3] Li KS, Guan Y, Wang J, et al. Genesis of a highly pathogenic and potentially pandemic H5N1 influenza virus in eastern Asia[J]. Nature, 2004, 430(6996), 209-213. [4] Couceiro JN, Paulson JC, Baum LG. Influenza virus strains selectively recognize sialyloligosaccharides on human respiratory epithelium;the role of the host cell in selection of hemagglutinin receptor specificity[J]. Virus Research, 1993, 29(2):155-165. [5] Yuan P, Bartlam M, Lou Z, et al. Crystal structure of an avian influenza polymerase PAN reveals an endonuclease active site[J]. Nature, 2009, 458(7240):909-913. [6] Liu Y, Lou Z, Bartlam M, et al. Structure-function studies of the influenza virus RNA polymerase PA subunit[J]. Science in China Series C:Life Sciences, 2009, 52(5):450-458. [7] Nistal-Villán E, et al. New prospects for the rational design of antivirals[J]. Nature Medicine, 2009, 15(11):1253-1254. [8] Crépin T, Dias A, et al. Mutational and metal binding analysis of the endonuclease domain of the influenza virus polymerase PA subunit[J]. Journal of Virology, 2010, 84(18):9096-9104. [9] Dias A, Bouvier D, Crépin T, et al. The cap-snatching endonuclease of influenza virus polymerase resides in the PA subunit[J]. Nature, 2009, 458(7240):914-918. [10] Sinev M, Landsmann P, Sineva E, et al. Design consideration and probes for fluorescence resonance energy transfer studies[J]. Bioconjugate Chemistry, 2000, 11, (3):352-362. [11] Gauglitz G, Proll G. Strategies for label-free optical detection[J]. Advances in Biochemical Engineering/Biotechnology, 2008, 109:395-432. [12] 徐筱杰, 侯廷军, 乔学, 等. 计算机辅助药物分子设计[M]. 北京:化学工业出版社, 2004. [13] 李洪林, 沈建华, 罗小民, 等. 虚拟筛选与新药发现[J]. 生命科学, 2005, 17(2):125-131. [14] Kowalinski E, Zubieta C, Wolkerstorfer A, et al. Structural analysis of specific metal chelating inhibitor binding to the endonuclease domain of influenza pH1N1(2009)Polymerase[J]. PLOS Pathogens, 2012, 8(8). e1002831.

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