Journal
BIOCONJUGATE CHEMISTRY
Volume 15, Issue 6, Pages 1464-1474Publisher
AMER CHEMICAL SOC
DOI: 10.1021/bc0498469
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Funding
- NCI NIH HHS [P50 CA94056] Funding Source: Medline
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Multidrug resistance (MDR) mediated by overexpression of MDR1 P-glycoprotein (Pgp) is one of the best characterized transporter-mediated barriers to successful chemotherapy in cancer patients. Thus, noninvasive interrogation of Pgp-mediated transport activity in vivo would be beneficial in guiding therapeutic choices. Both small organic medicinals as well as metal complexes characterized as transport substrates for Pgp are amenable to incorporation of PET or SPECT radionuclides and may enable noninvasive imaging of Pgp in cancer patients. Toward this objective, clinically approved agents, exemplified by Tc-99m-Sestamibi and (99m)Tetrofosmin, have already shown promise for the functional evaluation of Pgp-mediated transport activity in human tumors in vivo. In addition, selected agents from an upcoming class of substituted Schiff-base gallium(III) complexes containing an N4O2 donor core in their organic scaffold and capable of generating both SPECT and PET radiopharmaceuticals have also been shown to be promising for noninvasive assessment of Pgp activity in vitro and in vivo.
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