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OCT1 was shown recently to be the rate-determining step in the clearance of several drugs in humans.
OCT1 modulates multiple cardiometabolic traits through effects on hepatic thiamine content.
Contrasting results have been reported on the role of rs628031 and rs683369 polymorphisms of SLC22A1 and rs776746 of CYP3A5 on imatinib treatment response in patients with chronic myeloid leukemia. The present meta-analysis supports the association of SLC22A1 and CYP3A5 genotypes with clinical imatinib response rates of chronic myeloid leukemia patients. [review]
Two SNPs and two insertions/deletions were detected in exon 7 of SLC22A1. For exon 7, 1222AA carriers together with the presence of both the 8-bp insertion and 3-bp deletion, and M420del alleles showed higher possibility of developing resistance towards Imatinib mesylate (IM)treatment. Our results warrant the need of genotyping this SNP in terms of modulating IM treatment in chronic myeloid leukaemia patients.
data indicate that OCT1 may contribute to uptake metformin and regulate pancreatic stellate cells (PSCs) activity. OCT1 is a target of metformin in regulating PSCs activity.
Treatment with peroxisome proliferator activated receptor gamma (PPARgamma) ligands significantly alters organic cation transporter-1 (OCT-1) activity in BCR-ABL1+ chronic myeloid leukemia (CML) cell lines.
inhibitory potency for morphine uptake was affected by the OCT1*2 allele. OCT2 showed only a limited uptake of ranitidine that was not significantly affected by the Ala270Ser polymorphism
Results indicated that OCT1 rs628031 and ABCG2 rs2231142 were associated with plasma lamotrigine concentrations in Han Chinese patients with epilepsy.
The additional role of SLC22A1/OCT1 genetics in M1 exposure in neonates.
The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for ("squelching") SRC-1 coactivator.
Variants of SLC22A1 gene are associated with serum acylcarnitines and metabolic diseases.
Results indicate that the interaction between OCT1 and SERT genes might play an important role in metformin gastrointestinal intolerance.
summarize current understanding of human OCT1 transporter hepatic gene regulation and propose potential post-transcriptional regulation by predicted miRNAs.
The response to 6 months of metformin treatment (HbA1c , homeostasis model assessment for insulin resistance, fasting insulin, and glucose changes) did not differ between SLC22A1 wild-type subjects and carriers of presumably low-activity SLC22A1 alleles
we assessed the role of miR-21 in mediating renal cell carcinoma chemoresistance and further showed that miR-21 silencing significantly (1) increased chemosensitivity of paclitaxel, 5-fluorouracil, oxaliplatin, and dovitinib; (2) decreased expression of multi-drug resistance genes; and (4) increased SLC22A1/OCT1, SLC22A2/OCT2, and SLC31A1/CTR1 platinum influx transporter expression
This condensed chromatin structure is associated with binding of DNMT3B and decreased occupancy of OCT1 transcription factor at MAML2 enhancer, suggesting a role of DNMT3B in increasing methylation of MAML2 after stilbenoid treatment.
genetic association studies in population of patients newly diagnosed type 2 diabetes in Bosnia and Herzegovina: Data suggest that genetic variations in OCT1 [R61C (rs12208357); M420del (rs72552763)] are associated with severe intolerance/gastrointestinal side effects due to metformin use in patients with type 2 diabetes.
This study indicates a promising role for intratumoral OCT1 mRNA expression as a prognostic biomarker in therapeutic algorithms in HCC
Data show that bisindolylmaleimides (BIMs) Ro 31-8220 also blocks activity of the solute carrier organic cation transporter 1 (OCT1), involved in uptake of marketed drugs in the liver, in a protein kinase C (PKC)-independent manner.
Homozygous carriers of the polymorphic OCT1 C-allele had no metformin-related toxicity as compared with 41.9% for any metformin-related toxicity in carriers of at least one wild-type A-allele
Dopamine transport across the olfactory and respiratory mucosae is partially mediated by organic cation transporters, including OCT-1 and OCT-2.
we unraveled substrate affinities and modulation of transport activity by acute regulation by protein kinases on mOCT1 and mOCT2
Data indicate that the expression of the organic cation transporters Slc22a1, Slc22a2 and Slc22a3 essential for the cellular uptake of metformin was highly suppressed in Tsc1+/-renal tumours.
Transcripts encoding OCT1-3 and ChAT (choline acetyltransferase) have been detected in tracheal epithelial cells; these data suggest that cells lining the airway are able to synthesize/secrete acetylcholine into the lumen.
The influence of organic cation transporters 1, 2, and 3 (OCT1, OCT2, and OCT3) and their genetic variants on cellular uptake of picoplatin and on the individual components of the ensuing cytotoxicity such as DNA adduct formation, was determined.
Oct1 forms repeating, cyclosporin-sensitive regulatory modules within the CD21 intronic control region.
rOCT1 could transport the nucleoside analog deoxytubercidin
Involvement in hepatic and intestinal distribution of metformin.
a comparison of the transport properties of Oct2 and Oct1
oct1 has a role in controlling fgl2 expression in endothelial cells
This study shows that Oct1 and Oct2 together are essential for renal secretion of (small) organic cations.
nuclear factor Y and Oct-1 bind to the SURG-1 element to direct basal and gonadotropin-releasing hormone (GnRH)-stimulated expression of the mGnRH receptor gene
The purpose of this study was to examine the effects of peroxisome proliferator agonist receptor agonists on the hepatic regulation and function of Slc22a1.
a multiprotein complex containing GATA-1, Oct-1, and other protein factors may contribute to the formation of a repressive chromatin structure that silences gamma-globin gene expression
Oct-1 has an important role in IFN-A regulation
Doubling of airway epithelial acetylcholine (ACh) in OCT1/2-/- mice is consistent with OCT1 and/or 2 mediating ACh release from respiratory epithelium. This effect does not contribute to 5-HT-induced constriction of murine intrapulmonary bronchi.
The ubiquitous Oct-1 transcription factor may be involved in hormonally regulated, tissue-specific beta-casein gene expression.
Real-time RT-PCR revealed significant decreases in OCT1 mRNA in the lung of sensitized and allergen challenged animals.
Genetic variation in OCT1 may contribute to variation in individual response to the drug.
Effect of OCT1 genotype on metformin pharmacokinetics in mice was less than in humans.
Polyspecific organic cation transporters in the liver, kidney, intestine, and other organs are critical for elimination of many endogenous small organic cations as well as a wide array of drugs and environmental toxins. This gene is one of three similar cation transporter genes located in a cluster on chromosome 6. The encoded protein contains twelve putative transmembrane domains and is a plasma integral membrane protein. Two transcript variants encoding two different isoforms have been found for this gene, but only the longer variant encodes a functional transporter.
solute carrier family 22 member 1
, solute carrier family 22 (organic cation transporter), member 1
, solute carrier family 22 member 1-like
, organic cation transporter 1
, solute carrier family 22, member 1
, solute carrier family 22 (organic cation transporter), member 2