The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery

[1]  V A Levin,et al.  Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability. , 1980, Journal of medicinal chemistry.

[2]  Yoko Shibata,et al.  Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor , 2008, Proceedings of the National Academy of Sciences.

[3]  P. Strange,et al.  Mechanisms of inverse agonist action at D2 dopamine receptors , 2005, British journal of pharmacology.

[4]  Charles C. Persinger,et al.  How to improve R&D productivity: the pharmaceutical industry's grand challenge , 2010, Nature Reviews Drug Discovery.

[5]  Brian K. Kobilka,et al.  Structural Instability of a Constitutively Active G Protein-coupled Receptor , 1997, The Journal of Biological Chemistry.

[6]  C. Tate,et al.  Transferability of thermostabilizing mutations between β-adrenergic receptors , 2009, Molecular membrane biology.

[7]  David G Myszka,et al.  Analyzing ligand and small molecule binding activity of solubilized GPCRs using biosensor technology. , 2006, Analytical biochemistry.

[8]  Michelle A. Schmidt,et al.  To Market, To Market—2004 , 2005 .

[9]  D. Colquhoun,et al.  Binding, gating, affinity and efficacy: The interpretation of structure‐activity relationships for agonists and of the effects of mutating receptors , 1998, British journal of pharmacology.

[10]  S. Kapur,et al.  Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis. , 2001, The American journal of psychiatry.

[11]  György M. Keserü,et al.  The influence of lead discovery strategies on the properties of drug candidates , 2009, Nature Reviews Drug Discovery.

[12]  David Colquhoun,et al.  The Relation between Classical and Cooperative Models for Drug Action , 1973 .

[13]  Arthur Christopoulos,et al.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders , 2009, Nature Reviews Drug Discovery.

[14]  Christopher G Tate,et al.  Development and crystallization of a minimal thermostabilised G protein-coupled receptor. , 2009, Protein expression and purification.

[15]  R. Henderson,et al.  Protein conformational changes in the bacteriorhodopsin photocycle. , 1999, Journal of molecular biology.

[16]  Miles Congreve,et al.  The impact of GPCR structures on pharmacology and structure‐based drug design , 2010, British journal of pharmacology.

[17]  T. Witek,et al.  Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease. , 1999, Life sciences.

[18]  T. Unger.  Differences Among Angiotensin II Type 1 Receptor Blockers: Characteristics of Candesartan Cilexetil , 2000, Blood pressure.

[19]  C. Tate,et al.  Engineering G protein-coupled receptors to facilitate their structure determination. , 2009, Current opinion in structural biology.

[20]  Christopher J Langmead,et al.  Muscarinic acetylcholine receptors as CNS drug targets. , 2008, Pharmacology & therapeutics.

[21]  K. Comess,et al.  An Ultraefficient Affinity-Based High-Throughout Screening Process: Application to Bacterial Cell Wall Biosynthesis Enzyme MurF , 2006, Journal of biomolecular screening.

[22]  V. Hornak,et al.  Light activation of rhodopsin: insights from molecular dynamics simulations guided by solid-state NMR distance restraints. , 2010, Journal of molecular biology.

[23]  G. Privé,et al.  Detergents for the stabilization and crystallization of membrane proteins. , 2007, Methods.

[24]  Yoko Shibata,et al.  Conformational thermostabilization of the β1-adrenergic receptor in a detergent-resistant form , 2008, Proceedings of the National Academy of Sciences.

[25]  Yoko Shibata,et al.  Thermostabilisation of the neurotensin receptor NTS1 , 2009, Journal of molecular biology.

[26]  Xavier Deupi,et al.  Conformational complexity of G-protein-coupled receptors. , 2007, Trends in pharmacological sciences.

[27]  M. Morelli,et al.  Adenosine A2A receptors and Parkinson's disease. , 2009, Handbook of experimental pharmacology.

[28]  R. Copeland,et al.  Drug–target residence time and its implications for lead optimization , 2007, Nature Reviews Drug Discovery.

[29]  Mark E Schurdak,et al.  Affinity-based screening techniques for enhancing lead discovery. , 2004, Current opinion in drug discovery & development.

[30]  C. Tate.  Practical considerations of membrane protein instability during purification and crystallisation. , 2010, Methods in molecular biology.

[31]  M. Caron,et al.  Regulation of beta-adrenergic receptors by guanyl-5'-yl imidodiphosphate and other purine nucleotides. , 1976, The Journal of biological chemistry.

[32]  L. Pardo,et al.  Ligand-specific regulation of the extracellular surface of a G protein coupled receptor , 2009, Nature.

[33]  G. Stephens.  G-protein-coupled-receptor-mediated presynaptic inhibition in the cerebellum. , 2009, Trends in pharmacological sciences.

[34]  P. Jacqmin,et al.  Population pharmacokinetic/pharmacodynamic analysis of CCR5 receptor occupancy by maraviroc in healthy subjects and HIV-positive patients. , 2008, British journal of clinical pharmacology.

[35]  Rich,et al.  Implementing surface plasmon resonance biosensors in drug discovery. , 2000, Pharmaceutical science & technology today.