Docking Simulations and in Vitro Assay Unveil Potent Inhibitory Action of Papaverine against Protein Tyrosine Phosphatase 1B(Pharmacology)

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概要

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• 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 (IC_<50>=1.20μM). 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.

• 2009-04-01

著者

• Taha Mutasem

  Faculty Of Pharmacy University Of Jordan

• BUSTANJI Yasser

  Faculty of Pharmacy, University of Jordan

• AL-MASRI Ihab

  Faculty of Pharmacy, Applied Science Private University

• MOHAMMAD Mohammad

  Faculty of Pharmacy, University of Jordan

• Al-masri Ihab

  Faculty Of Pharmacy Applied Science Private University:faculty Of Pharmacy Al-azhar University

• Bustanji Yasser

  Faculty Of Pharmacy University Of Jordan:faculty Of Pharmacy Applied Science Private University

• Mohammad Mohammad

  Faculty Of Pharmacy University Of Jordan

関連論文

• Docking Simulations and in Vitro Assay Unveil Potent Inhibitory Action of Papaverine against Protein Tyrosine Phosphatase 1B(Pharmacology)

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