ArticleBritish journal of pharmacology2011
Protein kinase C regulates the internalization and function of the human organic anion transporting polypeptide 1A2.
Article in British journal of pharmacology, 2011. 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, 50 citations in OpenAlex.
- Organic anion transporting polypeptides: Pharmacology, toxicology, structure, and transport mechanisms.Pharmacological reviews · 2025Review
- Subcellular activation of β-adrenergic receptors using a spatially restricted antagonist.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- The Role of CYPs and Transporters in the Biotransformation and Transport of the Anti-hepatitis C Antiviral Agents Asunaprevir, Daclatasvir, and Beclabuvir: Impact of Liver Disease, Race and Drug-drug Interactions on Safety and Efficacy.Current drug metabolism · 2024Review
- Is It Time to Use Modeling of Cellular Transporter Homeostasis to Inform Drug-Drug Interaction Studies: Theoretical Considerations.The AAPS journal · 2021Article
- Post-translational regulation of the major drug transporters in the families of organic anion transporters and organic anion-transporting polypeptides.The Journal of biological chemistry · 2020Review
- Trafficking and other regulatory mechanisms for organic anion transporting polypeptides and organic anion transporters that modulate cellular drug and xenobiotic influx and that are dysregulated in disease.British journal of pharmacology · 2017Review
- Cyanobacterial Toxins of the Laurentian Great Lakes, Their Toxicological Effects, and Numerical Limits in Drinking Water.Marine drugs · 2017Review
- Endocytosis of tight junction proteins and the regulation of degradation and recycling.Annals of the New York Academy of Sciences · 2017Review
- Protein Kinases C-Mediated Regulations of Drug Transporter Activity, Localization and Expression.International journal of molecular sciences · 2017Review
- Downregulation of Organic Anion Transporting Polypeptide (OATP) 1B1 Transport Function by Lysosomotropic Drug Chloroquine: Implication in OATP-Mediated Drug-Drug Interactions.Molecular pharmaceutics · 2016Article
- Human oligopeptide transporter 2 (PEPT2) mediates cellular uptake of polymyxins.The Journal of antimicrobial chemotherapy · 2016Article
- Human organic anion transporting polypeptide 1A2 (OATP1A2) mediates cellular uptake of all-trans-retinol in human retinal pigmented epithelial cells.British journal of pharmacology · 2015Article
- The altered renal and hepatic expression of solute carrier transporters (SLCs) in type 1 diabetic mice.PloS one · 2015Article
- Common mechanisms of Alzheimer's disease and ischemic stroke: the role of protein kinase C in the progression of age-related neurodegeneration.Journal of Alzheimer's disease : JAD · 2015Review
- Novel mechanism of impaired function of organic anion-transporting polypeptide 1B3 in human hepatocytes: post-translational regulation of OATP1B3 by protein kinase C activation.Drug metabolism and disposition: the biological fate of chemicals · 2014Article
- Article
- Organic anion-transporting polypeptides.Current topics in membranes · 2014Review
- Tumor-specific expression of organic anion-transporting polypeptides: transporters as novel targets for cancer therapy.Journal of drug delivery · 2013Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe human organic anion transporting polypeptide 1A2 (OATP1A2) is expressed in cells from several regions of the human body, including the kidney, cholangiocytes and the blood-brain barrier, and mediates the cellular flux of various anionic substances, including drugs in clinical use. Several related mammalian transporters have been shown to be subject to post-translational regulation, including kinase-induced internalization. In the present study the role of protein kinase C (PKC) in the regulation of OATP1A2 was investigated in an in vitro cell model. EXPERIMENTAL APPROACH: COS-7 cells in which OATP1A2 was overexpressed were treated with the PKC-specific activator (phorbol 12-myristate 13-acetate; PMA) and the PKC-specific inhibitor (Go6976). The impact of these treatments on the function and regulation of OATP1A2 was determined. KEY
resultsPKC activation decreased the transport function of OATP1A2 in a time- and concentration-dependent manner. PMA (0.1 µM) decreased the V(max) of oestrone-3-sulphate uptake and decreased the cell surface expression of OATP1A2 immunoreactive protein; these effects of PMA were prevented by the PKC specific inhibitor Go6976. In further studies, PMA treatment accelerated the internalization of OATP1A2 but did not affect its recycling. The disruption of clathrine-dependent endocytosis attenuated both the constitutive and PKC-modulated internalization of OATP1A2. In contrast, blocking the caveolin-dependent pathway was without effect. CONCLUSIONS AND IMPLICATIONS: PKC regulates the transport function of OATP1A2 by modulating protein internalization; this effect of PKC is mediated in part by clathrine-dependent pathways.
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