GPCR Drug Discovery | Publications

 

Article abstracts are available by clicking the journal reference and article reprints can be obtained by contacting us

Doré A. et al.
Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine
Structure (2011), doi:10.1016/j.str.2011.06.014

Zhukov A. et al.
Biophysical Mapping of Adenosine A2A Receptor (Article).
J. Med. Chem. 2011 DOI: 10.1021/jm2003798

Congreve M. et al.
Progress in Structure Based Drug Design for G Protein-Coupled Receptors (Perspective).
J. Med. Chem. 2011 DOI: 10.1021/jm200371q

Lebon G. et al.
Agonist-bound structures of the adenosine A2A reveals common features of GPCR activation.
Nature 2011 May

Congreve M, et al.
Fragment screening of stabilized G-protein-coupled receptors using biophysical methods.
Methods Enzymol.

Warne T, et al.
The structural basis for agonist and partial agonist action on a beta(1)-adrenergic receptor.
Nature. 2011 Jan 13;469(7329):241-244.

Robertson N, et al.
The properties of thermostabilised G protein-coupled receptors (StaRs®) and their use in drug discovery.
Neuropharmacology. 2011 Jan;60(1):36-44.

Hutchings CJ, Koglin M, and Marshall FH.
Therapeutic antibodies directed at G-protein-coupled receptors.
MAbs. 2010 Nov-Dec;2(6):594-606.

Marshall FH and Foord SM.
Heterodimerization of the GABAB receptor-implications for GPCR signaling and drug discovery.
Adv Pharmacol. 2010;58:63-91.

Tate CG and Stevens RC.
Growth and excitement in membrane protein structural biology.
Curr Opin Struct Biol. 2010 Aug;20(4):399-400.

Tate CG.
Biochemistry. Membrane protein gymnastics.
Science. 2010 Jun 25;328(5986):1644-1645.

Langmead C. 
Screening for allosteric modulators of G-protein-coupled receptors.
In: GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions
(2010) Annette Gilchrist (Editor) ISBN: 978-0-470-30778-6.

Errey JC and Marshall FH.
New techniques to express and crystallise G-protein coupled receptors
In: GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions
(2010) Annette Gilchrist (Editor) ISBN: 978-0-470-30778-6.

Congreve M and Marshall FH.
The impact of GPCR structures on pharmacology and structure- based drug design.
Br J Pharmacol. 2010 Mar;159(5):986-996.

Tate CG.
Practical considerations of membrane protein instability during purification and crystallisation.
Methods Mol Biol. 2010;601:187-203.

Serrano-Vega MJ and Tate CG.
Transferability of thermostabilizing mutations between beta-adrenergic receptors.
Mol Membr Biol. 2009 Dec;26(8):385-396.

Tate CG and Schertler GF.
Engineering G protein-coupled receptors to facilitate their structure determination.
Curr Opin Struct Biol. 2009 19(4); 386-395.

Shibata  Y, et al.
Thermostabilization of the neurotensin receptor NTS1.link
J Mol Biol. 2009 390(2); 262-277.

Serrano-Vega MJ, et al.
Conformational thermostabilization of the beta-1-adrenergic receptor in a detergent-resistant form.
PNAS. 2008 105(3); 877-882.

Warne T, et al.
Structure of a b1-adrenergic G-protein-coupled receptor.
Nature. 2008 454(7203); 486-491.

Magnani F, et al.
Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor.
PNAS. 2008 105(31); 10744-10749.

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Electron density around the cyanopindolol ligand binding site in the beta 1 adrenergic receptor.

Acknowledgements. Warne et al, Nature. 2008.

 

Target GPCR crystals grown by the lipidic cubic phase method at Heptares Therapeutics.

Acknowledgements. Andrew Doré, Heptares Therapeutics Ltd, UK.