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KMID : 0363820010350020066
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Korean Journal of Nuclear Medicine
2001 Volume.35 No. 2 p.66 ~ p.75
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Functional Imaging of the Multidrug Resistance In Vivo.
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이재태/Jae Tae Lee
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Abstract
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Although diverse mechanisms are involved in multidrug resistance for chemotherapeutic drugs, the development of cellular P-glycoprotein(Pgp) and multidrug-resistance associated protein (MRP) are important factors in the chemotherapy failure to
cancer.
Various detection assays provide information about the presence of drug efflux pumps at the mRNA and protein levels. However these methods do not yield information about dynamic function of Pgp and MRP in vivo. Single photon emission tomography
(SPECT)
and positron emission tomography (PET) are available for the detection of Pgp and MRP-mediated transport. 99mTc-sestaMIBI and other 99mTc- radiopharmaceuticals are substrates for Pgp and MRP, and have been used in clinical studies for tumor
imaging, and
to visualize blockade of Pgp-mediated transport after modulation of Pgp pump. Colchicine, verapamil and daunorubicin labeled with 11C have been evaluated for the quantification of Pgp-mediated transport with PET in vivo and reported to be
feasible
substrates with which to image Pgp function in tumors. Leukotrienes are specific substrates for MRP and N-[11C]acetyl-leukotriene E4 provides an opportunity to study MRP function non-invasively in vivo. Results obtained from recent publications
are
reviewed to confirm the feasibility of using SPECT and PET to study the functionality of MDR transporters in vivo.
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KEYWORD
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