Human OAT1, OAT3, OAT4 and OATP1A2 Facilitate the Renal Accumulation of Ochratoxin A [PDF]
PharmaceuticsBackground/Objectives: Ochratoxin A (OTA) is a widespread foodborne mycotoxin linked to chronic kidney disease of unknown etiology. Despite evidence from animal models showing OTA accumulation in the kidney, the molecular mechanisms underlying its renal ...
Anish Mahadeo +7 more
doaj +4 more sources
OATP1A2 mediates Aβ1-42 transport and may be a novel target for the treatment of Alzheimer’s disease [PDF]
Frontiers in PharmacologyAlzheimer’s disease (AD) is a neurodegenerative disease with an unknown cause. Many studies have suggested that the imbalance between the clearance and accumulation of β-amyloid protein (Aβ) in the brain of AD patients is the main cause of AD development
Jinhua Wen +4 more
doaj +4 more sources
Enhancing transporter activity in heterologous expression systems with SAHA: a 2500‐times more potent and odorless alternative to butyrate [PDF]
FEBS Open BioThe functional characterization of plasma membrane transport proteins often relies on their heterologous expression in cultured cells. However, some transporters exhibit low activity, hindering meaningful functional assays.
Svenja Flögel +4 more
doaj +3 more sources
PDZK1 and NHERF1 Regulate the Function of Human Organic Anion Transporting Polypeptide 1A2 (OATP1A2) by Modulating Its Subcellular Trafficking and Stability [PDF]
PLoS ONE, 2014 The human organic anion transporting polypeptide 1A2 (OATP1A2) is an important membrane protein that mediates the cellular influx of various substances including drugs. Previous studies have shown that PDZ-domain containing proteins, especially PDZK1 and
Zhou F, Michael Murray, Ling Zhu
exaly +6 more sources
Structural Dynamics of OATP1A2 in Mediating Paclitaxel Transport Mechanism in Breast Cancer [PDF]
NanotheranosticsBreast cancer remains a significant global health challenge, with drug resistance and poor bioavailability of chemotherapeutic agents like paclitaxel (PTX) presenting obstacles to effective treatment. This study investigates the potential role of the Solute Carrier Organic Anion Transporter Polypeptide 1A2 (OATP1A2) in PTX transport using computational
Kumar R +5 more
exaly +4 more sources
Polymorphisms in Human Organic Anion-transporting Polypeptide 1A2 (OATP1A2) [PDF]
Journal of Biological Chemistry, 2005 Organic anion-transporting polypeptide 1A2 (OATP1A2) is a drug uptake transporter known for broad substrate specificity, including many drugs in clinical use. Therefore, genetic variation in SLCO1A2 may have important implications to the disposition and tissue penetration of substrate drugs.
Wooin Lee +2 more
exaly +3 more sources
Environmental and Genetic Factors Affecting Transport of Imatinib by OATP1A2 [PDF]
Clinical Pharmacology and Therapeutics, 2011 The bioavailability of orally administered imatinib is >90%, although the drug is monocationic under the acidic conditions in the duodenum. In vitro, we found that imatinib is transported by the intestinal uptake carrier organic anion transporting polypeptide (OATP1A2) and that this process is sensitive to pH, rosuvastatin, and genetic variants ...
R H J Mathijssen +2 more
exaly +4 more sources
Endoxifen-glucuronide and 4-hydroxy-tamoxifen glucuronide are substrates of OATP1A2
ASPET DiscoveryTamoxifen is a widely prescribed antiestrogen for breast cancer therapy that undergoes P450-mediated formation of the active metabolites 4-hydroxy-tamoxifen (4-OH-tamoxifen) and endoxifen prior to glucuronidation. Organic anion-transporting polypeptides (
Michelle K. Wong +3 more
doaj +2 more sources
Functional Analysis of Novel Polymorphisms in the Human SLCO1A2 Gene that Encodes the Transporter OATP1A2 [PDF]
AAPS Journal, 2013 The solute carrier organic anion transporting polypeptide 1A2 (OATP1A2, SLCO1A2) is implicated in the cellular influx of a number of drugs. We identified five novel single nucleotide polymorphisms (SNPs) in coding exons of the SLCO1A2 gene in a cohort of subjects: G550A, G553A, G673A, A775C, and G862A, that encoded the OATP1A2 variants E184K, D185N ...
Zhou F, Michael Murray, W Bret Church
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Influence of Human OATP1B1, OATP1B3, and OATP1A2 on the Pharmacokinetics of Methotrexate and Paclitaxel in Humanized Transgenic Mice [PDF]
Clinical Cancer Research, 2013 Abstract Purpose: Organic anion-transporting polypeptide (OATP) drug uptake transporters are thought to play an important role in drug pharmacokinetics and toxicokinetics. We aimed to determine the influence of the individual human OATP1B1, OATP1B3, and OATP1A2 transporters on the in vivo disposition of the anticancer drugs ...
Alfred Schinkel +2 more
exaly +3 more sources