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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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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author Heather M. Bigott
Julie L. Prior
David R. Piwnica-Worms
Michael J. Welch
author_facet Heather M. Bigott
Julie L. Prior
David R. Piwnica-Worms
Michael J. Welch
author_sort Heather M. Bigott
collection DOAJ
description 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.
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spelling doaj-art-f73f8cbbafb24b7dae0e0012b3672f362025-01-02T22:37:02ZengSAGE PublishingMolecular Imaging1536-01212005-01-01410.1162/1535350020050416610.1162_15353500200504166Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-SestamibiHeather M. BigottJulie L. PriorDavid R. Piwnica-WormsMichael J. WelchThe 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.https://doi.org/10.1162/15353500200504166
spellingShingle Heather M. Bigott
Julie L. Prior
David R. Piwnica-Worms
Michael J. Welch
Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi
Molecular Imaging
title Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi
title_full Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi
title_fullStr Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi
title_full_unstemmed Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi
title_short Imaging Multidrug Resistance P-glycoprotein Transport Function Using MicroPET with Technetium-94m-Sestamibi
title_sort imaging multidrug resistance p glycoprotein transport function using micropet with technetium 94m sestamibi
url https://doi.org/10.1162/15353500200504166
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