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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.

P-glycoprotein ( Pgp) is one of the ABC transporters responsible for the multidrug resistance of cancer cells. The conformational changes of Pgp that occur in the presence of substrates/modulators or ATP depletion are accompanied by the up-shift of UIC2 monoclonal antibody (mAb) binding. In the case of cyclosporin A, vinblastine or valinomycin, this up-shift was found to be concomitant with the near-complete suppression of labeling with other mAbs specific for Pgp epitopes overlapping with UIC2, while pre-treatment with verapamil or Tween 80 brings about a modest suppression. Here we have extended these observations to 44 Pgp interacting agents, and found that only 8 fall into the cyclosporin-like category, inducing a conformational state characterized by the complete UIC2 dominance. The rest of the drugs either did not affect antibody competition or had a modest effect. Thus, Pgp substrates/modulators can be classified into distinct modalities based on the conformational change they elicit.[1]

References

  1. Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Nagy, H., Goda, K., Fenyvesi, F., Bacsó, Z., Szilasi, M., Kappelmayer, J., Lustyik, G., Cianfriglia, M., Szabó, G. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
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