Technetium-99m-Tetrofosmin Would Be a Substrate for Multidrug Resistance-associated Protein (MRP): Comparison between a Leukemia Cell Line with High MRP Gene Expression and Its Parental Cell Line

Cancer chemotherapy has been used since the early 1950s and still remains one the major therapeutic options for many malignant tumours. A major obstacle to successful cancer chemotherapy is drug resistance. Frequently resistance is intrinsic to the cancer, but as therapy becomes more effective, acquired resistance has also become more frequent. One form of resistance, named multidrug resistance (MDR), is responsible for the failure of tumours to respond to a wide spectrum of chemotherapeutic agents. The in vivo monitoring of MDR could assist in the selection of patients for therapy and can avoid ineffective and potentially toxic treatments. Therefore, methods for functionally interrogating MDR transport activity have been sought, namely single photon emission computed tomography (SPECT) and positron emission tomography (PET). Cationic radiotracers originally developed as SPECT myocardial imaging agents, such as [(99m)Tc(MIBI)(6)](+) and [(99m)Tc(tetrofosmin)(2)O(2)](+), are used for both early cancer detection and non-invasive monitoring of the tumour MDR transport function. With the ultimate goal of obtaining better performing radioprobes for MDR imaging, other metal-based complexes and/or small molecules have also been synthesized and biologically evaluated. In this perspective we will report on the chemical efforts made to find metalloprobes for in vivo monitoring of MDR by nuclear imaging techniques. The current knowledge on the biological mechanisms and proteins involved in tumour MDR will be also briefly presented, as its understanding is invaluable for the rational design and biological evaluation of new radioprobes.

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Technetium-99m-Tetrofosmin Would Be a Substrate for Multidrug Resistance-associated Protein (MRP): Comparison between a Leukemia Cell Line with High MRP Gene Expression and Its Parental Cell Line

Abstract: 99mTc-TF would be a substrate for MRP and 99mTc-TF may be used as a functional imaging agent of MRP in vivo.

Cited by 9 publications

References 14 publications

Attempts to Image MRP1 Function in the Blood-Brain Barrier Using the Metabolite Extrusion Method

Attempts to Image MRP1 Function in the Blood-Brain Barrier Using the Metabolite Extrusion Method

Expression of multidrug resistance-associated protein (MRP) and its relationship with clinicopathological factors in non-small cell lung cancer

Metalloprobes for functional monitoring of tumour multidrug resistance by nuclear imaging

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