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03/2012
A large number of G-protein-coupled receptors (GPCRs) show varying degrees of basal or constitutive activity. This constitutive activity is usually minimal in... 
Constitutive activity | inverse agonists | G-protein-coupled receptors | inverse agonism
Web Resource
Journal Article
Cell Metabolism, ISSN 1550-4131, 08/2012, Volume 16, Issue 2, pp. 167 - 179
Journal Article
LIFE SCIENCES, ISSN 0024-3205, 02/2005, Volume 76, Issue 12, pp. 1307 - 1324
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 07/2017, Volume 292, Issue 28, pp. 11618 - 11630
The nuclear receptor retinoid acid receptor-related orphan receptor gamma t (ROR gamma t) is a master regulator of the Th17/IL-17 pathway that plays crucial... 
CELLS | PROTEIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | SUSCEPTIBILITY | IDENTIFICATION | DISCOVERY | x-ray crystallography | retinoid acid receptor-related orphan receptor t (RORt) | drug discovery | protein drug interaction | nuclear magnetic resonance (NMR) | IL-17 | crystal structure | nuclear receptor | DIFFERENTIATION | LIGAND | BINDING | GENOME-WIDE ASSOCIATION | Apoproteins - chemistry | Nuclear Receptor Subfamily 1, Group F, Member 3 - antagonists & inhibitors | Phenylalanine - analogs & derivatives | Phenylalanine - pharmacology | Humans | Molecular Conformation | Th17 Cells - secretion | Anti-Inflammatory Agents, Non-Steroidal - chemistry | Recombinant Fusion Proteins - metabolism | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Th17 Cells - drug effects | Th17 Cells - metabolism | Phenylalanine - chemistry | Phenylurea Compounds - chemistry | Nuclear Receptor Subfamily 1, Group F, Member 3 - metabolism | HEK293 Cells | Phenylurea Compounds - metabolism | Protein Interaction Domains and Motifs | Anti-Inflammatory Agents, Non-Steroidal - metabolism | Protein Stability | Binding Sites | Peptide Fragments - genetics | Apoproteins - metabolism | Nuclear Receptor Subfamily 1, Group F, Member 3 - genetics | Binding, Competitive | Apoproteins - antagonists & inhibitors | Nuclear Receptor Subfamily 1, Group F, Member 3 - chemistry | Peptide Fragments - metabolism | Phenylalanine - metabolism | Interleukin-17 - secretion | Cells, Cultured | Protein Refolding | Models, Molecular | Recombinant Fusion Proteins - chemistry | Interleukin-17 - metabolism | Peptide Fragments - chemistry | Interleukin-17 - antagonists & inhibitors | Peptide Fragments - antagonists & inhibitors | Drug Inverse Agonism | Apoproteins - genetics | Genes, Reporter - drug effects | Ligands | Protein Conformation | Phenylurea Compounds - pharmacology | Index Medicus | Protein Structure and Folding | retinoid acid receptor-related orphan receptor γt (RORγt)
Journal Article
CELLULAR AND MOLECULAR LIFE SCIENCES, ISSN 1420-682X, 02/2019, Volume 76, Issue 3, pp. 561 - 576
P2Y(12) receptor (P2Y(12)-R) is one of the major targets for drug inhibiting platelet aggregation in the treatment/prevention of arterial thrombosis. However,... 
ACTIVATION | EFFICACY | Constitutive activity | BIOCHEMISTRY & MOLECULAR BIOLOGY | ADENOSINE | ADP | GENE POLYMORPHISM | CELL BIOLOGY | Aggregation | Platelet | INDUCED PLATELET-AGGREGATION | CLOPIDOGREL | INHIBITION | GPCR | LIGAND | SELECTIVITY
Journal Article
Indian Journal of Pharmacology, ISSN 0253-7613, 10/2011, Volume 43, Issue 5, pp. 492 - 501
Journal Article
Journal Article
PHARMACOLOGY & THERAPEUTICS, ISSN 0163-7258, 02/2009, Volume 121, Issue 2, pp. 160 - 173
Contemporary receptor theory was developed to account for the existence of constitutive activity, as defined by the presence of receptor signaling in the... 
Serotonin 5-HT2A receptor | PANIC DISORDER | Constitutive activity | Stimulus trafficking | FRONTAL-CORTEX | PROTEIN-COUPLED RECEPTORS | Inverse agonism | ELEVATED PLUS-MAZE | PREFRONTAL CORTEX | ATYPICAL ANTIPSYCHOTIC-DRUGS | SIGNAL-TRANSDUCTION | M-CHLOROPHENYLPIPERAZINE | Serotonin 5-HT2C receptor | IN-VIVO | PHARMACOLOGY & PHARMACY
Journal Article
PROCEEDINGS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES, ISSN 0962-8452, 06/2019, Volume 286, Issue 1904, pp. 20190884 - 20190884
Bitter taste enables the detection of potentially harmful substances and is mediated by bitter taste receptors, TAS2Rs, in vertebrates. Few antagonists and... 
REPERTOIRE | ANTAGONIST | inverse agonist | G-protein-coupled receptor | SENSITIVITY | molecular evolution | lemur | EVOLUTIONARY BIOLOGY | EVOLUTION | RANGES | DIET | BIOLOGY | ECOLOGY | BINDING | bitter taste receptor | INSIGHTS
Journal Article