Literature DB >> 9786024

Ligand-binding studies: old beliefs and new strategies.

G E Rovati1.   

Abstract

Ligand-binding studies remain a very popular technique among many experimentalists. As far as equilibrium experiments are concerned, saturation and displacement curves are commonly performed for simplicity, convenience or for the sake of tradition. However, alternative protocols, such as 'mixed'-type protocols or multiligand experiments, are also possible. Indeed, there are cases where kinetic experiments, usually considered a 'second-choice' experiment, might have a superior resolving power compared to equilibrium ones. A combination of equilibrium and kinetic experiments might be a powerful solution to overcome limits and shortcomings of each specific technique and is discussed in this issue by G. Enrico Rovati. Thus, a careful choice of the design, a protocol optimization and a computerized analysis of the data can yield a dramatic improvement in the precision of the parameter estimation over more conventional approaches.

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Year:  1998        PMID: 9786024     DOI: 10.1016/s0165-6147(98)01242-5

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN: 0165-6147            Impact factor:   14.819


  9 in total

1.  Superactive mutants of thromboxane prostanoid receptor: functional and computational analysis of an active form alternative to constitutively active mutants.

Authors:  Manuela Ambrosio; Francesca Fanelli; Silvia Brocchetti; Francesco Raimondi; Mario Mauri; G Enrico Rovati; Valérie Capra
Journal:  Cell Mol Life Sci       Date:  2010-04-11       Impact factor: 9.261

2.  Methodological comparison of in vitro binding parameter estimation: sequential vs. simultaneous non-linear regression.

Authors:  C Steven Ernest; Andrew C Hooker; Mats O Karlsson
Journal:  Pharm Res       Date:  2010-03-11       Impact factor: 4.200

Review 3.  Ligand binding assays at equilibrium: validation and interpretation.

Authors:  Edward C Hulme; Mike A Trevethick
Journal:  Br J Pharmacol       Date:  2010-11       Impact factor: 8.739

4.  Radioligand saturation binding for quantitative analysis of ligand-receptor interactions.

Authors:  Chengyan Dong; Zhaofei Liu; Fan Wang
Journal:  Biophys Rep       Date:  2016-02-14

5.  Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators.

Authors:  Jan Jakubík; Alena Randáková; Esam E El-Fakahany; Vladimír Doležal
Journal:  PLoS One       Date:  2019-03-27       Impact factor: 3.240

6.  Design and validation of recombinant protein standards for quantitative Western blot analysis of cannabinoid CB1 receptor density in cell membranes: an alternative to radioligand binding methods.

Authors:  Miquel Saumell-Esnaola; Ainhoa Elejaga-Jimeno; Leyre Echeazarra; Leire Borrega-Román; Sergio Barrondo; Maider López de Jesús; Imanol González-Burguera; Alberto Gómez-Caballero; María Aranzazu Goicolea; Joan Sallés; Gontzal García Del Caño
Journal:  Microb Cell Fact       Date:  2022-09-15       Impact factor: 6.352

7.  Full and partial agonists of thromboxane prostanoid receptor unveil fine tuning of receptor superactive conformation and G protein activation.

Authors:  Valérie Capra; Marta Busnelli; Alessandro Perenna; Manuela Ambrosio; Maria Rosa Accomazzo; Celine Galés; Bice Chini; G Enrico Rovati
Journal:  PLoS One       Date:  2013-03-28       Impact factor: 3.240

8.  CysLT1 receptor-induced human airway smooth muscle cells proliferation requires ROS generation, EGF receptor transactivation and ERK1/2 phosphorylation.

Authors:  Saula Ravasi; Simona Citro; Barbara Viviani; Valérie Capra; G Enrico Rovati
Journal:  Respir Res       Date:  2006-03-22

9.  Reduced ligand affinity leads to an impaired function of the adenosine A2A receptor of human granulocytes in sepsis.

Authors:  Simone Kreth; Ines Kaufmann; Carola Ledderose; Benjamin Luchting; Manfred Thiel
Journal:  J Cell Mol Med       Date:  2009-05       Impact factor: 5.310

  9 in total

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