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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
medicine
Berberine potently inhibits protein tyrosine phosphatase 1B: Investigation by docking simulation and experimental validation
Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 21, No. 2, Year 2006
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Description
Berberine was investigated as an inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B) in an attempt to explain its anti-hyperglycemic activitiy. The investigation included simulated docking experiments to fit berberine within the binding pocket of h-PTP 1B. Berberine was found to readily fit within the binding pocket of h-PTP 1B in a low energy orientation characterized with optimal electrostatic attractive interactions bridging the isoquinolinium positively charged nitrogen atom of berberine and the negatively charged acidic residue of ASP 48 of h-PTP 1B. Experimentally, berberine was found to potently competitively inhibit recombinant h-PTP 1B in vitro (Ki value = 91.3 nM). Our findings strongly suggest that h-PTP 1B inhibition is at least one of the reasons for the reported anti-hyperglycemic activities of berberine. © 2006 Taylor & Francis.
Authors & Co-Authors
Bustanji, Yasser Khalil
Jordan, Amman
The University of Jordan
Taha, Mutasem O.
Jordan, Amman
The University of Jordan
Yousef, Al Motassem F.
Jordan, Amman
The University of Jordan
Al-Bakri, Amal G.
Jordan, Amman
The University of Jordan
Statistics
Citations: 37
Authors: 4
Affiliations: 1
Identifiers
Doi:
10.1080/14756360500533026
ISSN:
14756366
e-ISSN:
14756374