Literature DB >> 20977467

Matching models to data: a receptor pharmacologist's guide.

David A Hall1, Christopher J Langmead.   

Abstract

UNLABELLED: In this review we discuss a number of topics related to fitting mechanistic mathematical models to experimental data. These can be divided broadly into issues to consider before beginning an experiment or fitting a model and the advantages of direct fitting of a model over other methods of analysis (e.g. null methods). We have sought to address some commonplace issues of receptor pharmacology with some real-life examples: How should dilutions be distributed along a concentration-response curve? How do problems with dilutions manifest in assay results? What assumptions are made when certain analysis models are applied? What is global data fitting and how does it work? How can it be applied to improve data analysis? How can models such as one-site and two-site fits be compared? What is the principal behind statistical comparison of data fits? It is our hope that after reading this review you will have a greater appreciation of assay planning and subsequent data analysis and interpretation which will improve the quality of the data that you generate. 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.
© 2010 The Authors. British Journal of Pharmacology © 2010 The British Pharmacological Society.

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Year:  2010        PMID: 20977467      PMCID: PMC3000653          DOI: 10.1111/j.1476-5381.2010.00879.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  21 in total

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Review 3.  Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors.

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  13 in total

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Review 3.  Efficacy and ligand bias at the μ-opioid receptor.

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Journal:  Br J Pharmacol       Date:  2013-08       Impact factor: 8.739

Review 4.  100 years of modelling ligand-receptor binding and response: A focus on GPCRs.

Authors:  David B Finlay; Stephen B Duffull; Michelle Glass
Journal:  Br J Pharmacol       Date:  2020-02-28       Impact factor: 8.739

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Journal:  Mol Pharmacol       Date:  2011-05-20       Impact factor: 4.436

6.  Probing the CB1 Cannabinoid Receptor Binding Pocket with AM6538, a High-Affinity Irreversible Antagonist.

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7.  Allosteric transition: a comparison of two models.

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Journal:  BMC Pharmacol Toxicol       Date:  2013-01-08       Impact factor: 2.483

8.  Low affinity GPCRs for metabolic intermediates: challenges for pharmacologists.

Authors:  Nicola J Smith
Journal:  Front Endocrinol (Lausanne)       Date:  2012-01-13       Impact factor: 5.555

9.  Exploring conformational preferences of proteins: ionic liquid effects on the energy landscape of avidin.

Authors:  Talia A Shmool; Laura K Martin; Coby J Clarke; Liem Bui-Le; Karen M Polizzi; Jason P Hallett
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10.  Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H3 receptor for Prader-Willi Syndrome.

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