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Reducing GABA Receptors
A number of important drugs act on GABA A receptors, pentameric GABA-gated chloride channels assembled from among 19 known subunits. In trying to discover the roles in the brain of the subunits and their combinations, with the goal of developing more selective drugs, one tool has been to reduce expr...
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Published in: | Life Sciences 2003-08, Vol.73 (14), p.1741-1758 |
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description | A number of important drugs act on GABA
A receptors, pentameric GABA-gated chloride channels assembled from among 19 known subunits. In trying to discover the roles in the brain of the subunits and their combinations, with the goal of developing more selective drugs, one tool has been to reduce expression of the subunits and examine the functional consequences. After briefly examining the properties of GABA
A receptors, this review surveys the means available for receptor subunit reduction, and some of the observations to which their application has led. The methods discussed include radiation-induced deletion, gene knockout, knock-in mutations, antisense, ribozymes, RNA interference, dominant negative constructs, and transcriptional regulation, e.g., via decoy oligonucleotides. |
doi_str_mv | 10.1016/S0024-3205(03)00505-8 |
format | article |
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subjects | Animals Anxiolytic Benzodiazepine Brain - metabolism Brain - physiology Chromosome Deletion Drug development Gamma-aminobutyric acid Humans Knockdown Oligonucleotides, Antisense - pharmacology Protein Subunits Receptors, GABA - biosynthesis Receptors, GABA - genetics Receptors, GABA - metabolism Receptors, GABA - physiology Receptors, GABA-A - biosynthesis Receptors, GABA-A - genetics Receptors, GABA-A - metabolism Receptors, GABA-A - physiology RNA Interference Sedative Silencing |
title | Reducing GABA Receptors |
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