Common Drugs Inhibit Human Organic Cation Transporter 1 (OCT1)-Mediated Neurotransmitter Uptake
نویسندگان
چکیده
منابع مشابه
Cellular uptake of imatinib into leukemic cells is independent of human organic cation transporter 1 (OCT1).
PURPOSE In addition to mutated BCR-ABL1 kinase, the organic cation transporter 1 (OCT1, encoded by SLC22A1) has been considered to contribute to imatinib resistance in patients with chronic myeloid leukemia (CML). As data are conflicting as to whether OCT1 transports imatinib and may serve as a clinical biomarker, we used a combination of different approaches including animal experiments to elu...
متن کاملThe human organic cation transporter OCT1 mediates high affinity uptake of the anticancer drug daunorubicin
Anthracyclines such as daunorubicin are anticancer agents that are transported into cells, and exert cytotoxicity by blocking DNA metabolism. Although there is evidence for active uptake of anthracyclines into cells, the specific transporter involved in this process has not been identified. Using the high-grade serous ovarian cancer cell line TOV2223G, we show that OCT1 mediated the high affini...
متن کاملCancer Therapy: Preclinical Cellular Uptake of Imatinib into Leukemic Cells Is Independent of Human Organic Cation Transporter 1 (OCT1)
Purpose: In addition to mutated BCR-ABL1 kinase, the organic cation transporter 1 (OCT1, encoded by SLC22A1) has been considered to contribute to imatinib resistance in patients with chronic myeloid leukemia (CML). As data are conflicting as to whether OCT1 transports imatinib andmay serve as a clinical biomarker, we used a combination of different approaches including animal experiments to elu...
متن کاملRegulation of basal core promoter activity of human organic cation transporter 1 (OCT1/SLC22A1).
Human organic cation transporter 1 (OCT1/SLC22A1) plays important roles in the hepatic uptake of cationic drugs. The functional characteristics of this transporter have been well evaluated, but molecular information regarding transcriptional regulation is limited. In the present study, therefore, we examined the gene regulation of OCT1 gene focusing on basal core expression. An approximately 2....
متن کاملEffect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action.
Metformin is among the most widely prescribed drugs for the treatment of type 2 diabetes. Organic cation transporter 1 (OCT1) plays a role in the hepatic uptake of metformin, but its role in the therapeutic effects of the drug, which involve activation of AMP-activated protein kinase (AMPK), is unknown. Recent studies have shown that human OCT1 is highly polymorphic. We investigated whether OCT...
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ژورنال
عنوان ژورنال: Drug Metabolism and Disposition
سال: 2014
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.113.055095