Receptors as microprocessors: pharmacological nuance on metabotropic glutamate receptors 1alpha.
G protein-coupled receptors have revealed themselves to be complex information-processing units that may be exploited for subtle therapeutic signaling effects. Thus, ligands may not only turn receptors on and off, but may also select from their repertoire of signaling effects to further refine drug response.
Kenakin
Terry
T
Assay Development, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. terry.p.kenakin@gsk.com
D000494:Allosteric Regulation; D000818:Animals; D001665:Binding Sites; D002116:Calcitonin / Q000494:pharmacology; D020013:Calcium Signaling / Q000187:drug effects / Q000502:physiology*; D002460:Cell Line; D000242:Cyclic AMP / Q000502:physiology*; D019281:Dimerization; D043802:GTP-Binding Protein alpha Subunits, Gq-G11 / Q000502:physiology; D019205:GTP-Binding Protein alpha Subunits, Gs / Q000235:genetics / Q000502:physiology; D005682:Gadolinium / Q000494:pharmacology; D018698:Glutamic Acid / Q000494:pharmacology; D006801:Humans; D007668:Kidney; D008024:Ligands; D008954:Models, Biological; D011485:Protein Binding; D011487:Protein Conformation; D025941:Protein Interaction Mapping; D017434:Protein Structure, Tertiary; D018003:Receptors, Calcitonin / Q000235:genetics / Q000502:physiology; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000502:physiology*; D018094:Receptors, Metabotropic Glutamate / Q000819:agonists / Q000502:physiology*; D011993:Recombinant Fusion Proteins / Q000502:physiology; D015290:Second Messenger Systems / Q000187:drug effects / Q000502:physiology*; D013329:Structure-Activity Relationship; D013552:Swine; D014162:Transfection
D008024:Ligands; D018003:Receptors, Calcitonin; D043562:Receptors, G-Protein-Coupled; D018094:Receptors, Metabotropic Glutamate; D011993:Recombinant Fusion Proteins; C104077:metabotropic glutamate receptor type 1; D018698:Glutamic Acid; D002116:Calcitonin; D005682:Gadolinium; D000242:Cyclic AMP; D043802:GTP-Binding Protein alpha Subunits, Gq-G11; D019205:GTP-Binding Protein alpha Subunits, Gs