Search Results - "Bertheleme, Nicolas"
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1
Unlocking the secrets of the gatekeeper: Methods for stabilizing and crystallizing GPCRs
Published in Biochimica et biophysica acta (01-11-2013)“…G-protein coupled receptors (GPCRs) are integral membrane cell surface receptors with key roles in mediating the cellular responses to a wide range of…”
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2
Arginine 199 and leucine 208 have key roles in the control of adenosine A2A receptor signalling function
Published in PloS one (03-03-2014)“…One successful approach to obtaining high-resolution crystal structures of G-protein coupled receptors is the introduction of thermostabilising mutations…”
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3
Heterologous expression of G-protein-coupled receptors in yeast
Published in Methods in enzymology (2015)“…Heterologous yeast expression systems have been successfully used for the production of G-protein-coupled receptors (GPCRs) for both structural and functional…”
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4
Loss of constitutive activity is correlated with increased thermostability of the human adenosine A2A receptor
Published in British journal of pharmacology (01-07-2013)“…Background and Purpose Thermostabilization by mutagenesis is one method which has facilitated the determination of high‐resolution structures of the adenosine…”
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5
Production of stable membrane proteins for the development of biologics
Published in Acta crystallographica. Section A, Foundations and advances (26-05-2017)“…Abstract only…”
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6
Arginine 199 and Leucine 208 Have Key Roles in the Control of Adenosine A.sub.2A Receptor Signalling Function
Published in PloS one (03-03-2014)“…One successful approach to obtaining high-resolution crystal structures of G-protein coupled receptors is the introduction of thermostabilising mutations…”
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Journal Article -
7
Loss of constitutive activity is correlated with increased thermostability of the human adenosine A 2A receptor
Published in British journal of pharmacology (01-07-2013)Get full text
Journal Article -
8
Functional characterisation of a2a receptor thermostable mutants using a yeast signalling assay
Published 01-01-2014“…G-protein-coupled receptors (GPCR) are transmembrane proteins that play a crucial role in the communication of cells with their external environment. In the…”
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Dissertation -
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The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist
Published in Bioorganic & medicinal chemistry letters (01-04-2010)“…The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A PR is described. Associated structure–activity…”
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Radioligand binding analysis as a tool for quality control of GPCR production for structural characterization: adenosine A(2a)R as a template for study
Published in Current protocols in protein science (01-02-2012)“…Functional characterization of G protein-coupled receptors is essential to ascertain the suitability of a protein target for downstream studies and to help…”
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11
Purification of the human G protein-coupled receptor adenosine A(2a)R in a stable and functional form expressed in Pichia pastoris
Published in Current protocols in protein science (01-02-2012)“…The isolation of membrane proteins with the aim of producing highly pure, homogeneous, stable, and functional material remains challenging, and it is often…”
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Journal Article