Structural Features for Functional Selectivity at Serotonin Receptors
نویسندگان
چکیده
منابع مشابه
Structural features for functional selectivity at serotonin receptors.
Drugs active at G protein-coupled receptors (GPCRs) can differentially modulate either canonical or noncanonical signaling pathways via a phenomenon known as functional selectivity or biased signaling. We report biochemical studies showing that the hallucinogen lysergic acid diethylamide, its precursor ergotamine (ERG), and related ergolines display strong functional selectivity for β-arrestin ...
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Serotonin or 5-hydroxytryptamine (5-HT) regulates a wide spectrum of human physiology through the 5-HT receptor family. We report the crystal structures of the human 5-HT1B G protein-coupled receptor bound to the agonist antimigraine medications ergotamine and dihydroergotamine. The structures reveal similar binding modes for these ligands, which occupy the orthosteric pocket and an extended bi...
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Several groups have characterized the pharmacology of 4or 6 3 -containing GABAA receptors expressed in different cell systems. We have previously demonstrated that the pharmacological profiles of a series of GABAA receptor agonists are highly dependent on the subunit and little on the and subunits, so to further understand the contribution of the different subunits in the GABAA receptor complex...
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ژورنال
عنوان ژورنال: Science
سال: 2013
ISSN: 0036-8075,1095-9203
DOI: 10.1126/science.1232808