Monitoring multidrug resistance P-glycoprotein drug transport activity with single-photon emission computed tomography and positron emission tomography radiopharmaceuticals

Vijay Sharma, David Piwnica-Worms

Research output: Chapter in Book/Report/Conference proceedingChapter

17 Scopus citations

Abstract

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 and there is an expanding requirement to noninvasively interrogate Pgp transport activity in vivo. Both small organic medicinals as well as coordination compounds characterized as transport substrates for MDR1 Pgp are amenable to incorporation of positron emission tomography or single-photon emission computed tomography radionuclides and may enable noninvasive diagnostic imaging of MDR in cancer patients. In particular, several clinically approved [99mTc] complexes already show promise for the functional evaluation of MDR1 Pgp-mediated transport activity in human tumors in vivo.

Original languageEnglish (US)
Title of host publicationContrast Agents III
Subtitle of host publicationRadiopharmaceuticals From Diagnostics to Therapeutics
EditorsWerner Krauze
Pages155-178
Number of pages24
DOIs
StatePublished - Nov 17 2005
Externally publishedYes

Publication series

NameTopics in Current Chemistry
Volume252
ISSN (Print)0340-1022

Keywords

  • ATP-binding cassette transporters
  • Chemotherapeutic agents
  • Metal complexes
  • Multidrug resistance
  • P-glycoprotein
  • Positron emission tomography
  • Single-photon emission computed tomography

ASJC Scopus subject areas

  • General Chemistry

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