ArticleBritish journal of pharmacology2008
Cultured CD4T cells and primary human lymphocytes express hOATPs: intracellular accumulation of saquinavir and lopinavir.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 44 citations in OpenAlex.
- Review
- Pitavastatin Exerts Potent Anti-Inflammatory and Immunomodulatory Effects via the Suppression of AP-1 Signal Transduction in Human T Cells.International journal of molecular sciences · 2019Article
- Drug-transporter mediated interactions between anthelminthic and antiretroviral drugs across the Caco-2 cell monolayers.BMC pharmacology & toxicology · 2017Article
- Antiretroviral drug transporters and metabolic enzymes in human testicular tissue: potential contribution to HIV-1 sanctuary site.The Journal of antimicrobial chemotherapy · 2016Article
- HIV-1 Alters Intestinal Expression of Drug Transporters and Metabolic Enzymes: Implications for Antiretroviral Drug Disposition.Antimicrobial agents and chemotherapy · 2016Article
- Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals.AIDS research and treatment · 2016Review
- Pharmacokinetic and pharmacodynamic drug interactions between antiretrovirals and oral contraceptives.Clinical pharmacokinetics · 2015Review
- Article
- Article
- Influence of drug transport proteins on the pharmacokinetics and drug interactions of HIV protease inhibitors.Journal of pharmaceutical sciences · 2011Review
- Exposure to HIV-protease inhibitors selects for increased expression of P-glycoprotein (ABCB1) in Kaposi's sarcoma cells.British journal of cancer · 2011Article
- Interactions of tenofovir, Lamivudine, abacavir and Didanosine in primary human cells.Pharmaceutics · 2011Article
- Concentration-dependent effects and intracellular accumulation of HIV protease inhibitors in cultured CD4 T cells and primary human lymphocytes.The Journal of antimicrobial chemotherapy · 2010Article
- Review
- The accumulation and metabolism of zidovudine in 3T3-F442A pre-adipocytes.British journal of pharmacology · 2010Article
- Montelukast is a potent and durable inhibitor of multidrug resistance protein 2-mediated efflux of taxol and saquinavir.Biological & pharmaceutical bulletin · 2009Article
- The role of transporters in the pharmacokinetics of orally administered drugs.Pharmaceutical research · 2009Review
- Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC.British journal of clinical pharmacology · 2009Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeDrug efflux tranporters (P-glycoprotein (P-gp), multidrug resistance-associated protein (MRP)) limit the cellular uptake of human immunodeficiency virus protease inhibitors but the contribution of influx transporters in cells that (over)express P-gp or MRP is less clear. Here, we studied the expression of one influx transporter system, human organic anion-transporting polypeptide (hOATP), in some T-cell lines (CEM, CEM(VBL), CEM(E1000)) and in peripheral blood mononuclear cells (PBMCs) and examined the effects of manipulation of influx/efflux transporters on the uptake of saquinavir and lopinavir. EXPERIMENTAL APPROACH: The expression of hOATPs was studied by PCR. We used hOATP substrate or inhibitor (estrone-3-sulphate (E-3-S) or montelukast, respectively) and inhibitors of P-gp (XR9576) and MRP (MK571 and frusemide) to study functional interactions between influx and efflux transporters in the uptake of saquinavir and lopinavir. Lipophilicity of the drugs was measured by octanol/saline partition coefficient. KEY
resultsCEM cells, their variants and PBMCs express various hOATP isoforms, with OATP3A1 detected in all of the cells. MK571, XR9576 and frusemide increased the uptake of saquinavir and lopinavir. E-3-S and montelukast reduced the uptake of saquinavir and lopinavir in some, but not all, of the cells. Pretreatment of the cells with MK571, XR9576 or frusemide, followed by E-3-S co-incubation reduced the cellular accumulation of saquinavir and lopinavir. Lopinavir is much more lipophilic than saquinavir. CONCLUSIONS AND IMPLICATIONS: Human OATPs, MRP, P-gp and lipophilicity determine the cellular uptake and retention of saquinavir and lopinavir. These data may have important implications for drug-drug interactions, drug safety and efficacy.
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