Functional Imaging of Multidrug Resistance and Its Applications


The emergence of multidrug resistance (MDR) is a major obstacle to the success of antineoplastic therapies [1]. The classical mechanism underlying MDR is the overexpression of energy-dependent transmembrane proteins behaving as drug efflux pumps. Three main proteins stand out in this family, P-glycoprotein (Pgp), multidrug resistance-associated protein-1 (MRP1), and breast cancer-related protein (BCRP). Each of these transporters has the ability to confer resistance to a broad spectrum of hydrophobic chemotherapeutic agents as a result of enhanced drug efflux [2]. These pumps, in particular Pgp, have been found in several highly resistant solid and hematological tumors and are associated with a poor prognosis [3–6]. Strategies to circumvent MDR include the co-administration of modulators, compounds that inhibit the functional activity of MDR-related transporters, and the use of cytotoxic agents that bypass the efflux mechanism [7]. Information on the functional expression of MDR-related transporters has the ability to provide a rational basis for developing potentially effective therapies that can be used in patients who are likely to be poor responders to standard chemotherapy and therefore have a poor prognosis under these circumstances.


Positron Emission Tomography Standardize Uptake Value Positron Emission Tomography Imaging Breast Cancer Resistance Protein Washout Rate 
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© Springer Science+Business Media, LLC 2009

Authors and Affiliations

  1. 1.Institute of Biophysics/Biomathematics, IBILI – Faculty of MedicineUniversity of CoimbraQueryPortugal

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