Forschungsdatenbank PMU-SQQUID

P-glycoprotein, multidrug resistance-associated proteins and human organic anion transporting polypeptide influence the intracellular accumulation of atazanavir.
Janneh, O; Anwar, T; Jungbauer, C; Kopp, S; Khoo, SH; Back, DJ; Chiba, P;
Antivir Ther. 2009; 14(7):965-974
Originalarbeiten (Zeitschrift)

Abstract/Keywords Web of Science PubMed Full Text

PMU-Autor/inn/en

Jungbauer Christof

Abstract

Drug efflux (for example, P-glycoprotein [P-gp], multidrug resistance-associated proteins [MRPs] and breast cancer resistance protein [BCRP]) and influx (for example, human organic anion transporting polypeptide [hOCTP] or human organic anion transporting polypeptide [hOATP]) transporters alter the cellular concentrations of some HIV protease inhibitors (HPIs). Here, we studied the lipophilicity and uptake of [(3)H]-atazanavir (ATV) in CEM (parental), CEM(VBL) (P-gp-overexpressing), CEM(E1000) (MRP1-overexpressing) and peripheral blood mononuclear cells (PBMCs), and evaluate the effects of modulators of drug transporters on uptake.

Useful keywords (using NLM MeSH Indexing)

ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists*

inhibitors

ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism*

Anti-HIV Agents/pharmacokinetics*

Atazanavir Sulfate

Biological Transport/drug effects

CD4-Positive T-Lymphocytes/drug effects

CD4-Positive T-Lymphocytes/metabolism

Cell Line

Digitonin/pharmacology

HIV Infections/drug therapy

HIV Infections/metabolism*

Humans

Indicators and Reagents/pharmacology

Intracellular Space/metabolism

Leukocytes, Mononuclear/drug effects

Leukocytes, Mononuclear/metabolism

Membrane Transport Modulators/pharmacology

Multidrug Resistance-Associated Proteins/antagonists*

inhibitors

Multidrug Resistance-Associated Proteins/metabolism*

Oligopeptides/pharmacokinetics*

Organic Anion Transporters/antagonists*

inhibitors

Organic Anion Transporters/metabolism*

Pyridines/pharmacokinetics*