Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery
نویسندگان
چکیده
منابع مشابه
Considerations in the evaluation of inverse agonism and protean agonism at G protein-coupled receptors.
Over the past decade it has become accepted that G protein-coupled receptors (GPCRs) can activate G proteins and thus initiate signaling in the absence of agonist; this spontaneous receptor activity can be inhibited to varying degrees by antagonists, a phenomenon termed inverse ugonism. The modulation of spontaneous GPCR activity by the binding of specific ligands implies that receptors can int...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2000
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0703311