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  • 标题:Docking Simulations and in Vitro Assay Unveil Potent Inhibitory Action of Papaverine against Protein Tyrosine Phosphatase 1B
  • 本地全文:下载
  • 作者:Yasser Bustanji ; Mutasem Omar Taha ; Ihab Mustafa Al-masri
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2009
  • 卷号:32
  • 期号:4
  • 页码:640-645
  • DOI:10.1248/bpb.32.640
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The structural similarity between papaverine and berberine, a known inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B), prompted us to investigate the potential of papaverine as h-PTP 1B inhibitor. The investigation included simulated docking experiments to fit papaverine into the binding pocket of h-PTP 1B. Papaverine was found to readily dock within the binding pocket of h-PTP 1B in a low energy orientation via an optimal set of attractive interactions. Experimentally, papaverine illustrated potent in vitro inhibitory effect against recombinant h-PTP 1B (IC50=1.20 μ M ). In vivo , papaverine significantly decreased fasting blood glucose level of Balb/c mice. Our findings should encourage screening of other natural alkaloids for possible anti-h-PTP 1B activities.
  • 关键词:papaverine;tyrosine phosphatase;human protein tyrosine phosphatase 1B;hypoglycemic activity;diabetes mellitus;docking simulation
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