Pharmacophore modelling of stereoselective binding to the human organic cation transporter (hOCT1)
نویسندگان
چکیده
منابع مشابه
Pharmacophore modelling of stereoselective binding to the human organic cation transporter (hOCT1).
BACKGROUND AND PURPOSE The human organic cation transporter-1 (hOCT1) is a polyspecific transporter that plays a role in drug distribution, metabolism and excretion. Previous studies have demonstrated that hOCT1 binding can be stereoselective, but the mechanism for stereochemical recognition has not been described. The purpose of this study was to develop a pharmacophore model to describe stere...
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Organic cation transporters play a critical role in the elimination of therapeutic compounds in the liver and the kidney. We used computational quantitative structure activity approaches to predict molecular features that influence interaction with the human ortholog of the organic cation transporter (hOCT1). [(3)H]tetraethylammonium uptake in HeLa cells stably expressing hOCT1 was inhibited to...
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Polyspecific organic cation transporters in epithelia play an important role in the elimination of many endogenous bioactive amines and therapeutically important drugs. Recently, the first human organic cation transporter (hOCT1) was cloned from liver. The purpose of the current study was to determine the effect of molecular size and hydrophobicity on the transport of organic cations by hOCT1. ...
متن کاملDecreased function of genetic variants, Pro283Leu and Arg287Gly, in human organic cation transporter hOCT1.
We have evaluated the functional consequences of genetic variations in human organic cation transporter hOCT1 (SLC22A1). Three coding single nucleotide polymorphisms (cSNPs) resulted in the amino acid changes Pro283Leu, Arg287Gly and Pro341Leu were assessed. Uptake experiments with transient expression system using HEK293 cells revealed that the variants Pro283Leu and Arg287Gly had completely d...
متن کاملFunctional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
Recently, a polyspecific organic cation transporter, hOCT1, was cloned from human liver. To date, limited studies examining the functional characteristics of the transporter have been performed. The purpose of the present study was to develop a mammalian expression system for hOCT1 and to characterize the interactions of various compounds with the cloned transporter. Lipofection was used to tra...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2007
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0707341