Multidrug resistance protein 1-mediated transport of saquinavir by microglia

Shannon Dallas, Patrick T. Ronaldson, Moise Bendayan, Reina Bendayan

Research output: Contribution to journalArticle

33 Scopus citations

Abstract

Regulation of CNS distribution of the human immunodeficiency virus (HIV) protease inhibitor saquinavir may involve ATP-dependent membrane-bound efflux transport proteins that are expressed in several brain cellular compartments. We recently characterized molecular and functional expression of one such transporter, multidrug resistance protein-1 (MRPI) in microglia, the primary brain cellular target of HIV. In the present study, we further examine subcellular localization of MRPI in a microglia cell line (MLS-9) using immunogold cytochemistry and directly demonstrate MRPI-mediated export of saquinavir. MRPI localized primarily to the plasma membrane of the MLS-9 cells. [14C]Saquinavir efflux by MLS-9 monolayers was inhibited by well-established MRPI inhibitors. These results indicate that MRPI contributes, in part, to the overall low permeation of protease inhibitors in the brain.

Original languageEnglish (US)
Pages (from-to)1183-1186
Number of pages4
JournalNeuroReport
Volume15
Issue number7
DOIs
StatePublished - May 19 2004
Externally publishedYes

Keywords

  • Brain transport
  • Human immunodeficiency virus
  • Microglia
  • Multidrug resistance protein 1
  • Saquinavir

ASJC Scopus subject areas

  • Neuroscience(all)

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