The evasive nature of drug efficacy: implications for drug discovery
S Galandrin, G Oligny-Longpré, M Bouvier - Trends in pharmacological …, 2007 - cell.com
The efficacy of a drug is generally determined by the drug's ability to promote a quantifiable
biological response. In the context of the classical receptor-occupancy theory, the efficacy is …
biological response. In the context of the classical receptor-occupancy theory, the efficacy is …
Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors
E Hermans - Pharmacology & therapeutics, 2003 - Elsevier
For decades, it has been generally proposed that a given receptor always interacts with a
particular GTP-binding protein (G-protein) or with multiple G-proteins within one family …
particular GTP-binding protein (G-protein) or with multiple G-proteins within one family …
Aripiprazole has functionally selective actions at dopamine D2 receptor-mediated signaling pathways
JD Urban, GA Vargas, M Von Zastrow… - …, 2007 - nature.com
Aripiprazole is a unique atypical antipsychotic drug with an excellent side-effect profile
presumed, in part, to be due to lack of typical D 2 dopamine receptor antagonist properties …
presumed, in part, to be due to lack of typical D 2 dopamine receptor antagonist properties …
RNA‐editing of the 5‐HT2C receptor alters agonist‐receptor‐effector coupling specificity
KA Berg, JD Cropper, CM Niswender… - British journal of …, 2001 - Wiley Online Library
The serotonin2C (5‐HT2C) receptor couples to both phospholipase C (PLC)‐inositol
phosphate (IP) and phospholipase A2 (PLA2)‐arachidonic acid (AA) signalling cascades …
phosphate (IP) and phospholipase A2 (PLA2)‐arachidonic acid (AA) signalling cascades …
Gonadotropin-Releasing Hormone (GnRH) Antagonists Promote Proapoptotic Signaling in Peripheral Reproductive Tumor Cells by Activating a Gαi-Coupling State …
S Maudsley, L Davidson, AJ Pawson, R Chan… - Cancer research, 2004 - AACR
Gonadotropin-releasing hormone (GnRH) receptor agonists are extensively used in the
treatment of sex hormone-dependent cancers via the desensitization of pituitary …
treatment of sex hormone-dependent cancers via the desensitization of pituitary …
Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays
SJ Charlton, G Vauquelin - British journal of pharmacology, 2010 - Wiley Online Library
Calcium is a key intracellular signal that controls manifold cellular processes over a wide
temporal range. The development of calcium‐sensitive fluorescent dyes and proteins …
temporal range. The development of calcium‐sensitive fluorescent dyes and proteins …
[引用][C] International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative …
RR Neubig, M Spedding, T Kenakin… - Pharmacological …, 2003 - ASPET