Results 1 to 10 of about 1,270 (136)

OATP1A2 mediates Aβ1-42 transport and may be a novel target for the treatment of Alzheimer’s disease [PDF]

Frontiers in Pharmacology
Alzheimer’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, Menghua Zhao
exaly   +6 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   +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 Bio
The 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, Maurice Tust, Samira Boussettaoui, Dietmar Fischer, Dirk Gründemann   +4 more
doaj   +3 more sources

OATP1A2 mRNA downregulation in canine hepatocellular carcinoma. [PDF]

Vet Rec Open
Abstract Background On gadolinium ethoxybenzyl diethylenetriamine pentaacetic acid (Gd‐EOB‐DTPA) magnetic resonance imaging, canine hepatocellular carcinoma (HCC) and hepatocellular adenoma (HCA) typically exhibit low and high signal intensities in the hepatobiliary phase, respectively.
Kurokawa S, Motegi T, Akiyoshi H, Tanaka T.   +3 more
europepmc   +2 more sources

Human OAT1, OAT3, OAT4 and OATP1A2 Facilitate the Renal Accumulation of Ochratoxin A [PDF]

Pharmaceutics
Background/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, Yik Pui Tsang, Angela R. Zheng, Sydney Arnzen, Acilegna G. Rodriguez, Mark S. Warren, Zsuzsanna Gáborik, Edward J. Kelly   +7 more
doaj   +2 more sources

Identification of a Functional CYP2C8 Variant Allele that Alters Splicing, Reduces Protein Expression, and Increases Drug Exposure. [PDF]

Clin Pharmacol Ther
This study investigated genetic determinants of the pharmacokinetics of the CYP2C8 index drugs repaglinide and gemfibrozil, and their interaction in healthy participants. Sequencing data from a study with montelukast revealed a novel functional CYP2C8 allele (rs2071426, CYP2C8*19), predicted to create an intronic splice donor site.
Mykkänen AJH, Hirvensalo P, Klein K, Kaminska D, Grube M, Tapaninen T, Kiiski JI, Neuvonen M, Männistö VT, Pihlajamäki J, Tzvetkov M, Schwab M, Tornio A, Backman JT, Niemi M.   +14 more
europepmc   +2 more sources

Substituent Effects of Heptamethine Cyanine Dyes on Drug Uptake in Patient-Derived Glioma Cells. [PDF]

ChemMedChem
Glioblastoma (GBM) remains difficult to treat primarily due to tumor heterogeneity and the presence of the blood–brain barrier (BBB). This study demonstrates the in vitro activity of the pan‐kinase inhibitor crizotinib conjugated to BBB‐penetrating heptamethine cyanine dyes with diverse functional groups across four patient‐derived GBM cell lines ...
Dumo CJ, Choi PJ, Liu Y, Muhammad O, Correia JA, Dragunow M, Park TI, Jose J.   +7 more
europepmc   +2 more sources

Differential Expression Patterns of SLCO Solute Carriers in Human Breast Cancer Cell Lines and Tumour Samples. [PDF]

J Cell Mol Med
ABSTRACT The cellular uptake of nutrients essential for cell growth and survival is facilitated by solute carrier (SLC) transporters. Members of the SLCO subfamily of SLCs mediate the uptake of substrates relevant to breast cancer (BC), including steroid hormones and anticancer drugs.
Telfer-Sutherland R, Page L, Meeson A, Lowes S.   +3 more
europepmc   +2 more sources

Perinatal Maturation of Drug Transporters and Claudin-5 at the Blood-Brain Barrier. [PDF]

CNS Neurosci Ther
P‐gp expression in the developping human cortex increases with age. In the mouse, gatekeepers of BBB integrity and transport are upregulated: tighter blood–brain barrier, increased claudin 5/Slco1a4/P‐gp expression as well as enhanced P‐gp‐mediated BBB efflux.
Federici L, Cisternino S, Auvity S, Gelot A, Becmeur-Lefebvre M, Favier M, Letort G, Mailly P, Cohen-Salmon M, Boulay AC.   +9 more
europepmc   +2 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]

Pharmaceutics
Background: 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, Lijun Luo, Ziqian Zhang, Xiao Liu, Naihong Chen, Yan Li, Li Sheng   +6 more
doaj   +2 more sources