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
Jian Zheng, Ting Chan, Ling Zhu
exaly +10 more sources
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 +3 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
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
Fanfan Zhou, Ling Zhu, Howard P Gurney
exaly +7 more sources
The Active Glucuronide Metabolite of the Brain Protectant IMM-H004 with Poor Blood–Brain Barrier Permeability Demonstrates a High Partition in the Rat Brain via Multiple Mechanisms [PDF]
PharmaceuticsBackground: Glucuronidation is an essential metabolic pathway for a variety of drugs. IMM-H004 is a novel neuroprotective agent against ischemic stroke, and its glucuronide metabolite IMM-H004G exhibits similar pharmacological activity.
Jianwei Jiang +6 more
doaj +2 more sources
Subcellular activation of β-adrenergic receptors using a spatially restricted antagonist. [PDF]
Proc Natl Acad Sci U S AGprotein-coupled receptors (GPCRs) regulate several physiological and pathological processes and represent the target of approximately 30% of Food and Drug Administration-approved drugs.
Liccardo F +6 more
europepmc +3 more sources
Molecules, 2021 In this study, we investigated the delivery of synthetic neurosteroids into MCF-7 human breast adenocarcinoma cells via Organic Anionic Transporting Polypeptides (OATPs) (pH 7.4 and 5.5) to identify the structural components required for OATP-mediated ...
Santosh Kumar Adla +5 more
doaj +1 more source
Identification of novel cell-impermeant fluorescent substrates for testing the function and drug interaction of Organic Anion-Transporting Polypeptides, OATP1B1/1B3 and 2B1. [PDF]
, 2018 Organic Anion-Transporting Polypeptides are multispecific membrane proteins that regulate the passage of crucial endobiotics and drugs across pharmacological barriers. OATP1B1 and OATP1B3 have been described to play a major role in the hepatic uptake of
Bakos, Éva +8 more
core +5 more sources
Estrone-3-sulphate, a potential novel ligand for targeting breast cancers. [PDF]
PLoS ONE, 2013 The current study investigates the potential of estrone-3-sulphate (E3S) as a ligand for targeting Organic Anion Transporting Polypeptides (OATP), a family of membrane associated uptake transporters, for detection and diagnosis of hormone dependent ...
Nilasha Banerjee +5 more
doaj +1 more source