Dopamine Transporter Ligand Binding Domains
نویسندگان
چکیده
منابع مشابه
Ligand binding by TPR domains.
Tetratricopeptide repeat (TPR) domains bind specific peptide ligands and are thought to mediate protein-protein interactions in a variety of biological systems. Here we compare peptide ligand-binding by several different TPR domains. We present specific examples that demonstrate that TPR domains typically undergo little or no structural rearrangement upon ligand binding. Our data suggest that, ...
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DAT inhibitors have at least two different binding mechanisms (Scheme 1): fast ligand binding following the conventional equilibrium scheme (i) and their binding effectiveness is described by the KA values; two-step binding, after initial fast binding step the ligand induces protein conformation change (ii) [2]. This extra step consists of a slow protein conformational change, enhancing the app...
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UNLABELLED 18F-labeled 2 beta-carbomethoxy-3beta-(4-chlorophenyl)-8-(-2-fluoroethyl)nortropane ([18F]FECNT) is a recently developed dopamine transporter ligand with potential applications in patients with Parkinson's disease and cocaine addiction. METHODS Estimates of the effective dose equivalent and doses for specific organs were made using biodistribution data from 16 Sprague-Dawley rats a...
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The neuronal dopamine transporter (DAT) is a major determinant of extracellular dopamine (DA) levels and is the primary target for a variety of addictive and therapeutic psychoactive drugs. DAT is acutely regulated by protein kinase C (PKC) activation and amphetamine exposure, both of which modulate DAT surface expression by endocytic trafficking. In order to use live imaging approaches to stud...
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Cocaine blocks the normal role of the dopamine transporter (DAT) in terminating dopamine signaling and in restricting its spatial spread through molecular interactions that remain largely obscure. Cocaine analog structure-activity studies suggest roles for cationic and hydrophobic interactions between DAT, dopamine, cocaine, and the sodium and chloride ions whose gradients power uptake processe...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1996
ISSN: 0021-9258
DOI: 10.1074/jbc.271.35.21672