GPCR Drug Discovery | Publications

 

Full articles (indicated with an asterisk) and abstracts are available by clicking the journal reference. Article reprints can be obtained by contacting us


Mason, J.S., et al.
New Insights from Structural Biology into the Druggability of G Protein-coupled Receptors
Trends Pharmacol. Sci. 2012, 10.1016/j.tips.2012.02.005

*Langmead, C. et al.
Identification of Novel Adenosine A2A Receptor Antagonists by Virtual Screening
J. Med. Chem. 2012, 55(5):1904–1909.

*Congreve, M. et al.
Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug Design
J. Med. Chem. 2012, 55 (5):1898–19034

Doré A. et al.
Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine
Structure. 2011, 7;19(9):1283-1293.

*Zhukov A. et al.
Biophysical Mapping of Adenosine A2A Receptor (Article).
 J. Med. Chem. 2011, 14;54(13):4312-4323.

*Congreve M. et al.
Progress in Structure Based Drug Design for G Protein-Coupled Receptors (Perspective).
 J. Med. Chem. 2011, 14;54(13):4283-4311.

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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The adenosine A2A receptor (shown here as a bundle of helical ribbons) is presented on the surface of many neuronal cells. Molecules known to bind to the A2A receptor include xanthines, such as caffeine (shown here as ball and stick models), and modified xanthines have been developed as potential treatments for neurodegenerative disorders such as Parkinson’s disease. Generation of an adenosine A2A StaR® led to the determination of its structure with caffeine bound, allowing visualisation of the interactions between caffeine and its receptor, and enabling potential new therapeutic molecules to be discovered.

Structure, Volume 19, Issue 9, Doré A.S. et al. Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine. Pp 1283-1293. Copyright Elsevier Ltd. All rights reserved. (2011)


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.