The news correspondents obtained a quote from the research, "Molecular modeling of these alkaloids docked to a homology model of Pgp was employed to optimize ligand-protein interactions and design analogues with increased affinity to Pgp. Moreover, the compounds were evaluated for their (1) binding affinity to Pgp by fluorescence quenching, and (2) MDR reversal activity using a panel of in vitro and cell-based assays and compared to verapamil, a known inhibitor of Pgp activity. Compound 7 revealed the highest affinity to Pgp of all Strychnos congeners (K-d = 4.4 mu M), the strongest inhibition of Pgp ATPase activity, and the strongest MDR reversal effect in two Pgp-expressing cell lines."
According to the news reporters, the research concluded: "Altogether, our findings suggest the clinical potential of these synthesized compounds as viable Pgp modulators justifies further investigation."
For more information on this research see: Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication. Bioorganic & Medicinal Chemistry, 2014;22(3):1148-1155. Bioorganic & Medicinal Chemistry can be contacted at:
Our news journalists report that additional information may be obtained by contacting S. Munagala, US Army Med Res & Mat Command, Telemed & Adv Technol Res Center,
Keywords for this news article include: Cancer,
Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC
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