P-glycoprotein (ABCB1) activity decreases raltegravir disposition in primary CD4+P-gphigh cells and correlates with HIV-1 viral load

  title={P-glycoprotein (ABCB1) activity decreases raltegravir disposition in primary CD4+P-gphigh cells and correlates with HIV-1 viral load},
  author={Gerard Minuesa and Cristina Arimany-Nard{\'i} and Itziar Erkizia and Samandhy Cedeño and Jos{\'e} Molt{\'o} and Bonaventura Clotet and Marçal Pastor-Anglada and Javier Martinez-Picado},
  journal={Journal of Antimicrobial Chemotherapy},
  pages={2782 - 2792}
Objectives To evaluate the role of P-glycoprotein (P-gp) and multidrug-resistant-protein 1 (MRP1) on raltegravir intracellular drug disposition in CD4+ T cells, investigate the effect of HIV-1 infection on P-gp expression and correlate HIV-1 viraemia with P-gp activity in primary CD4+ T cell subsets. Methods The cellular accumulation ratio of [3H]raltegravir was quantified in CD4+ T cell lines overexpressing either P-gp (CEM-P-gp) or MRP1 (CEM-MRP1) and in primary CD3+CD4+ T cells with high (P… 

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