ArticleAIDS research and human retroviruses2014
Expression and localization of p-glycoprotein, multidrug resistance protein 4, and breast cancer resistance protein in the female lower genital tract of human and pigtailed macaque.
Article in AIDS research and human retroviruses, 2014. 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, 26 citations in OpenAlex.
- Single-dose pharmacokinetics of tenofovir alafenamide and its active metabolite in the mucosal tissues.The Journal of antimicrobial chemotherapy · 2017Trial
- Trial
- Expanding the Gene Expression Profiling of Drug Transporters and Drug-Metabolizing Enzymes to Include the Upper Female Reproductive Tract.Pharmaceutics · 2026Article
- In Vitro Pharmacokinetic Properties of MK-2048, a Potent Drug Candidate for HIV Prevention.Viruses · 2026Article
- Pharmacological evaluation of an ex vivo cervicovaginal HIV prevention model.The Journal of antimicrobial chemotherapy · 2026Article
- Female Reproductive Tract Organ-on-Chips: Modeling Barrier Function and Drug Transport.Pharmaceutics · 2026Review
- Vaginal pharmacomicrobiomics modulates risk of persistent and recurrent bacterial vaginosis.NPJ biofilms and microbiomes · 2025Review
- Drug transporter mRNA expression and genital inflammation in South African women on oral pre-exposure prophylaxis (PrEP).AIDS research and therapy · 2025Article
- Transport and Permeation Properties of Dapivirine: Understanding Potential Drug-Drug Interactions.Pharmaceutics · 2022Article
- Comprehensive Study of Antiretroviral Drug Permeability at the Cervicovaginal MucosaPharmaceutics · 2022Article
- Expression, Activity, and Regulation of Phosphorylating Enzymes in Tissues and Cells Relevant to HIV-1 Sexual Transmission.AIDS research and human retroviruses · 2022Article
- Multidrug efflux transporter ABCG2: expression and regulation.Cellular and molecular life sciences : CMLS · 2021Review
- The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics:Frontiers in pharmacology · 2019Review
- Pharmacology of Antiretrovirals in the Female Genital Tract for HIV Prevention.Journal of clinical pharmacology · 2018Review
- Expression, regulation, and function of drug transporters in cervicovaginal tissues of a mouse model used for microbicide testing.Biochemical pharmacology · 2016Article
- Cervicovaginal and Rectal Fluid as a Surrogate Marker of Antiretroviral Tissue Concentration: Implications for Clinical Trial Design.Journal of acquired immune deficiency syndromes (1999) · 2016Article
- Drug transporters in tissues and cells relevant to sexual transmission of HIV: Implications for drug delivery.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- Expression of Genes for Drug Transporters in the Human Female Genital Tract and Modulatory Effect of Antiretroviral Drugs.PloS one · 2015Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
Antiretroviral drug absorption and disposition in cervicovaginal tissue is important for the effectiveness of vaginally or orally administered drug products in preexposure prophylaxis (PrEP) of HIV-1 sexual transmission to women. Therefore, it is imperative to understand critical determinants of cervicovaginal tissue pharmacokinetics. This study aimed to examine the mRNA expression and protein localization of three efflux transporters, P-glycoprotein (P-gp), multidrug resistance-associated protein 4 (MRP4), and breast cancer resistance protein (BCRP), in the lower genital tract of premenopausal women and pigtailed macaques. Along the human lower genital tract, the three transporters were moderately to highly expressed compared to colorectal tissue and liver, as revealed by real-time reverse transcriptase polymerase chain reaction (RT-PCR). In a given genital tract segment, the transporter with the highest expression level was either BCRP or P-gp, while MRP4 was always expressed at the lowest level among the three transporters tested. The immunohistochemical staining showed that P-gp and MRP4 were localized in multiple cell types including epithelial cells and vascular endothelial cells. BCRP was predominantly localized in the vascular endothelial cells. Differences in transporter mRNA level and localization were observed among endocervix, ectocervix, and vagina. Compared to human tissues, the macaque cervicovaginal tissues displayed comparable expression and localization patterns of the three transporters, although subtle differences were observed between the two species. The role of these cervicovaginal transporters in drug absorption and disposition warrants further studies. The resemblance between human and pigtailed macaque in transporter expression and localization suggests the utility of the macaque model in the studies of human cervicovaginal transporters.
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