Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi

The best characterized mechanism of multidrug resistance (MDR) in cancer involves the MDR1 efflux transporter P-glycoprotein (Pgp). The positron-emitting radiotracer hexakis (2-methoxyisobutylisonitrile)- 94m Tc ( 94m Tc-MIBI) was synthesized and validated in cell transport studies as a substrate fo...

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Bibliographic Details
Main Authors: Heather M. Bigott, Julie L. Prior, David R. Piwnica-Worms, Michael J. Welch
Format: Article
Language:English
Published: SAGE Publishing 2005-01-01
Series:Molecular Imaging
Online Access:https://doi.org/10.1162/15353500200504166
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Summary:The best characterized mechanism of multidrug resistance (MDR) in cancer involves the MDR1 efflux transporter P-glycoprotein (Pgp). The positron-emitting radiotracer hexakis (2-methoxyisobutylisonitrile)- 94m Tc ( 94m Tc-MIBI) was synthesized and validated in cell transport studies as a substrate for MDR1 Pgp. In vivo small-scale PET imaging and biodistribution studies of mdr1a/1b (−/−) gene deleted and wild-type mice demonstrated the use of 94m Tc-MIBI to detect Pgp function. The reversal effect of a Pgp modulator was shown in tissue distribution studies of KB 3–1 (Pgp-) and KB 8–5 (Pgp+) tumor-bearing nude mice. The current 94m Tc-MIBI experiments parallel previous studies employing 99m Tc-MIBI, showing essentially identical performance of the two technetium radiotracers and providing biological validation of 94m Tc-MIBI for PET imaging of multidrug resistance.
ISSN:1536-0121