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

Clinical Pharmacokinetic and Metabolism of PET Radiotracers for Imaging P-glycoprotein in Chemoresistant Tumor of Colorectal Cancer.

The pharmacological treatment of colorectal tumour leads to MultiDrug Resistance due to overexpression of several ABC transporters such as P-glycoprotein and some Multidrug associated Resistance Proteins (MRPs) that are able to efflux the chemotherapeutic agent out of the cell. A strategy to reverse MDR is the co-administration of antineoplastic agent with a P-glycoprotein inhibitor. These inhibitors are an useful tool for investigating, by PET, the expression and the activity of P-gp and MRPs that are overexpressed in chemoresistant colorectal tumor cells. In this review will be focused the aspect on P-gp and MRPs ligands employed as PET radiotracers considering their pharmacokinetic pharmacodynamic profile and their selectivity towards ABC transporters involved in chemoresistant cell of colorectal tumour.[1]

References

  1. Clinical Pharmacokinetic and Metabolism of PET Radiotracers for Imaging P-glycoprotein in Chemoresistant Tumor of Colorectal Cancer. Cantore, M., Capparelli, E., Berardi, F., Perrone, R., Colabufo, N.A. Curr. Drug Metab. (2011) [Pubmed]
 
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