ReviewBritish journal of pharmacology2010
Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors.
Review in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed.
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- A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.Journal of medicinal chemistry · 2021Article
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- A Dynamic, Split-Luciferase-Based Mini-G Protein Sensor to Functionally Characterize Ligands at All Four Histamine Receptor Subtypes.International journal of molecular sciences · 2020Article
- Unique Pharmacological Properties of the Kappa Opioid Receptor Signaling Through GMolecular pharmacology · 2020Article
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- Comparisons of In Vivo and In Vitro Opioid Effects of Newly Synthesized 14-Methoxycodeine-6-Molecules (Basel, Switzerland) · 2020Article
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- Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.Journal of medicinal chemistry · 2019Article
- Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine AJournal of medicinal chemistry · 2019Article
- Efficacy-Based Perspective to Overcome Reduced Opioid Analgesia of Advanced Painful Diabetic Neuropathy in Rats.Frontiers in pharmacology · 2019Article
Corrections and comments
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Abstract
unlabelledIn this review I consider assays for G protein-coupled receptor (GPCR) activity based on the binding of labelled analogues of GTPγS ([(35) S]GTPγS or Eu-GTPγS) to G proteins in tissues (GTPγS binding assays). Such assays provide convenient measures of GPCR activity close to the receptor in the signalling cascade. In order to set up a GTPγS binding assay, the requirements of the assay must be considered. These are tissue source, GTPγS analogue, G protein, GDP, Mg(2+) /Na(+) ions, saponin, incubation time. The assay, once optimized, can be used to generate concentration/response curves for GPCRs signalling via G(i/o) proteins (or to other G proteins with a modified assay) and actions of agonists, inverse agonists and antagonists may, in principle, be assessed. For agonists and inverse agonists, data for the maximal agonist effect, the concentration of ligand giving a half-maximal response and the Hill coefficient may be derived. For antagonists, data for the equilibrium dissociation constant can be obtained. The mechanistic basis of the assay is considered. Although the assay can be used to profile ligands, under the conditions it is used, it may not be measuring the same event that determines GPCR action in cells. LINKED ARTICLES: This article is part of a themed section on Analytical Receptor Pharmacology in Drug Discovery. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2010.161.issue-6
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