Mechanisms of Sorafenib Resistance in HCC Culture Relate to the Impaired Membrane Expression of Organic Cation Transporter 1 (OCT1) [PDF]
Journal of Hepatocellular CarcinomaSrinivas Chava,1 Nergiz Ekmen,2 Pauline Ferraris,1 Yucel Aydin,2 Krzysztof Moroz,1 Tong Wu,1 Swan N Thung,3 Srikanta Dash1,2,4 1Department of Pathology and Laboratory Medicine, Tulane University Health Sciences Center, New Orleans, LA, USA; 2Department ...
Chava S +7 more
doaj +2 more sources
Expression status of p53 and organic cation transporter 1 is correlated with poor response to preoperative chemotherapy in esophageal squamous cell carcinoma [PDF]
World Journal of Surgical Oncology, 2022 Background Esophageal squamous cell carcinoma (ESCC) is a highly malignant neoplasm. DNA-damaging drugs, such as cisplatin (CDDP) and 5-fluorouracil (5-FU), are most frequently used in preoperative chemotherapy for ESCC.
Masahiro Izutsu +9 more
doaj +2 more sources
Metformin efficacy and tolerance according to genetic polymorphisms of organic cation transporter 1 in Tunisian patients with type 2 diabetes [PDF]
Frontiers in EndocrinologyPurposeMetformin efficacy and tolerance vary at equivalent dose in type 2 diabetes. Inter-individual variability in the response to metformin with approximately 35% of patients failing to achieve initial glycemic control may be explained by genetic ...
Fatma Chaker +7 more
doaj +2 more sources
Liver Fibrosis Stages Affect Organic Cation Transporter 1/2 Activities in Hepatitis C Virus-Infected Patients [PDF]
PharmaceuticalsThis study aims to evaluate the impact of liver fibrosis stages of chronic infection with hepatitis C virus (HCV) on the in vivo activity of organic cation transporters (hepatic OCT1 and renal OCT2) using metformin (MET) as a probe drug.
Matheus De Lucca Thomaz +7 more
doaj +2 more sources
Protein Kinase C-Independent Inhibition of Organic Cation Transporter 1 Activity by the Bisindolylmaleimide Ro 31-8220. [PDF]
PLoS ONE, 2015 Ro 31-8220 is a potent protein kinase C (PKC) inhibitor belonging to the chemical class of bisindolylmaleimides (BIMs). Various PKC-independent effects of Ro 31-8220 have however been demonstrated, including inhibition of the ATP-binding cassette drug ...
Abdullah Mayati +6 more
doaj +2 more sources
Organic cation transporter 1 (OCT1) is involved in pentamidine transport at the human and mouse blood-brain barrier (BBB). [PDF]
PLoS ONE, 2017 Pentamidine is an effective trypanocidal drug used against stage 1 Human African Trypanosomiasis (HAT). At the blood-brain barrier (BBB), it accumulates inside the endothelial cells but has limited entry into the brain.
Gayathri N Sekhar +7 more
doaj +2 more sources
Substrates of the Human Brain Proton-Organic Cation Antiporter and Comparison with Organic Cation Transporter 1 Activities. [PDF]
Int J Mol Sci, 2022 Many organic cations (OCs) may be transported through membranes by a genetically still uncharacterized proton-organic cation (H + OC) antiporter. Here, we characterized an extended substrate spectrum of this antiporter. We studied the uptake of 72 drugs in hCMEC/D3 cells as a model of the human blood–brain barrier.
Doetsch DA +6 more
europepmc +4 more sources
Relationships between Inhibition, Transport and Enhanced Transport via the Organic Cation Transporter 1. [PDF]
Int J Mol Sci, 2022 The organic cation transporter 1 (OCT1, SLC22A1) transports a large number of structurally diverse endogenous and exogenous substrates. There are numerous known competitive and non-competitive inhibitors of OCT1, but there are no studies systematically analyzing the relationship between transport, stimulation, and inhibition.
Jensen O +3 more
europepmc +5 more sources
Functional identification of organic cation transporter 1 as an atenolol transporter sensitive to flavonoids. [PDF]
Biochem Biophys Rep, 2015 Atenolol, a β1-adrenergic receptor blocker, is administered orally and its intestinal absorption has recently been indicated to be mediated by carrier protein and reduced markedly by ingestion of some fruit juices, such as apple and orange juices. This could be postulated to be a problem arising from the interaction of some components of fruit juices ...
Mimura Y +4 more
europepmc +3 more sources
Acta Pharmaceutica Sinica B, 2021 Disease-mediated alterations to drug disposition constitute a significant source of adverse drug reactions. Cisplatin (CDDP) elicits nephrotoxicity due to exposure in proximal tubule cells during renal secretion.
Joseph L. Jilek +6 more
doaj +1 more source