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Membrane transporters in drug development
TLDR
Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions, as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling. Expand
Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action.
TLDR
The data indicate that OCT1 is important for metformin therapeutic action and that genetic variation in OCT1 may contribute to variation in response to the drug. Expand
Sequence diversity and haplotype structure in the human ABCB1 (MDR1, multidrug resistance transporter) gene.
TLDR
This study represents a comprehensive analysis of ABCB1 nucleotide diversity and haplotype structure in different populations and illustrates the importance of haplotype considerations in characterizing the functional consequences ofABCB1 polymorphisms. Expand
Evolutionary conservation predicts function of variants of the human organic cation transporter, OCT1
TLDR
The results indicate that changes at evolutionarily conserved positions of OCT1 are strong predictors of decreased function and suggest that a combination of evolutionary conservation and chemical change might be a stronger predictor of function. Expand
The concentrative nucleoside transporter family, SLC28
TLDR
Nucleoside transporters in the SLC28 and SLC29 families play critical roles in nucleoside salvage pathways where they mediate the first step of nucleotide biosynthesis and work in concert to terminate adenosine signaling. Expand
Organic cation transporters are determinants of oxaliplatin cytotoxicity.
TLDR
The results indicate that OCT1 and OCT2 are major determinants of the anticancer activity of oxaliplatin and may contribute to its antitumor specificity and strongly suggest that expression of OCTs in tumors should be investigated as markers for selecting specific platinum-based therapies in individual patients. Expand
Cloning and functional expression of a human liver organic cation transporter.
TLDR
The functional expression of hOCT1 will provide a powerful tool for elucidation of the mechanisms of organic cation transport in the human liver and understanding of the mechanism involved in the disposition and hepatotoxicity of drugs. Expand
Emerging Transporters of Clinical Importance: An Update From the International Transporter Consortium
TLDR
Additional transporters of emerging importance in pharmacokinetics, interference of drugs with transport of endogenous compounds, and drug–drug interactions (DDIs) in humans are identified. Expand
Interaction of Methotrexate with Organic-Anion Transporting Polypeptide 1A2 and Its Genetic Variants
TLDR
The interaction of MTX with human organic-anion transporting polypeptide transporter (OATP) 1A2, which is expressed in tissues important for MTX disposition and toxicity, is characterized and suggests that OATP1A2 may play a role in active tubular reabsorption ofMTX and in MTX-induced toxicities. Expand
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
TLDR
Transiently transfected HeLa cells represent a useful tool in studying the interactions and kinetics of organic cations and other xenobiotics with hOCT1 and in understanding the molecular events involved in organic cation transport. Expand
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