Pradeep Nathan et al.

A phase 1b/2a multicentre study of the safety and preliminary pharmacodynamic effects of the selective muscarinic M1 receptor agonist HTL0018318 in patients with mild-to-moderate Alzheimer's disease

Alessandro Nicoli et al.

Classification Model for the Second Extracellular Loop of Class A GPCRs

Ian Winfield et al.

The Role of ICL1 and H8 in Class B1 GPCRs; Implications for Receptor Activation

Flavio Ballante et al.

Structure-Based Virtual Screening for Ligands of G Protein-Coupled Receptors: What Can Molecular Docking Do for You?

Alastair Brown et al.

From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease

Duuamene Nyimanu et al.

In vitro metabolism of synthetic Elabela/Toddler (ELA-32) peptide in human plasma and kidney homogenates analyzed with mass spectrometry and validation of endogenous peptide quantification in tissues by ELISA

Jon Palacios-Filardo et al.

Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits

Laura Jenkins et al.

Discovery and Characterization of Novel Antagonists of the Proinflammatory Orphan Receptor GPR84

Morgan Thomas et al.

Applications of Artificial Intelligence in Drug Design: Opportunities and Challenges

Miles Congreve et al.

Structure-Based Drug Design for G Protein-Coupled Receptors

Joshua Frenster et al.

Functional impact of intramolecular cleavage and dissociation of adhesion G protein-coupled receptor GPR133 (ADGRD1) on canonical signaling

Sean Colloby et al.

Spatial Covariance of Cholinergic Muscarinic M1 /M4 Receptors in Parkinson's Disease

Morgan Thomas et al.

Comparison of structure- and ligand-based scoring functions for deep generative models: a GPCR case study

Lisa Stott et al.

Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

Marton Vass et al.

Aminergic GPCR-Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data

Marta Arimont et al.

Chemokine Receptor Crystal Structures: What Can Be Learned from Them?

Ilze Adlere et al.

Modulators of CXCR4 and CXCR7/ACKR3 Function

Ali Işbilir et al.

Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists

David Favara et al.

Elevated expression of the adhesion GPCR ADGRL4/ELTD1 promotes endothelial sprouting angiogenesis without activating canonical GPCR signalling

Charlotte Bakker and Samantha Prins et al.

Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M1 acetylcholine receptor agonist: a randomized cross-over trial

Charlotte Bakker et al.

Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study

Inna Slynko et al.

Vanishing white matter: Eukaryotic initiation factor 2B model and the impact of missense mutations

Attila Egyed et al.

Controlling the selectivity of aminergic GPCR ligands from the extracellular vestibule

Tasia Amelia et al.

Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A2A Receptor

Sarah Baxendale et al.

The adhesion GPCR Adgrg6 (Gpr126): Insights from the zebrafish model

Kirstie Bennett et al.

Understanding exposure-receptor occupancy relationships for metabotropic glutamate receptor 5 (mGlu5) negative allosteric modulators across a range of pre-clinical and clinical studies

Georgi Kanev et al.

KLIFS: an overhaul after the first 5 years of supporting kinase research

Sangbae Lee et al.

How Do Branched Detergents Stabilize GPCRs in Micelles?

Joshua Frenster et al.

Expression profiling of the adhesion G protein-coupled receptor GPR133 (ADGRD1) in glioma subtypes

Matilda Shackley et al.

Short Chain Fatty Acids Enhance Expression and Activity of the Umami Taste Receptor in Enteroendocrine Cells via a Gα i/o Pathway

Anna Delamarre et al.

Gastrointestinal and metabolic function in the MPTP-treated macaque model of Parkinson's disease

Charlotte Bakker et al.

First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1‐receptor partial agonist for the treatment of Dementias

Pradeep Nathan and Geor Bakker

Lessons learned from using fMRI in the early clinical development of a mu-opioid receptor antagonist for disorders of compulsive consumption

James Errey and Cedric Fiez-Vandal

Production of membrane proteins in industry: The example of GPCRs

Martha Sommer et al.

The European Research Network on Signal Transduction (ERNEST): Toward a Multidimensional Holistic Understanding of G Protein-Coupled Receptor Signaling

Kirstie Bennett et al.

Structure-based discovery and development of metabotropic glutamate receptor 5 negative allosteric modulators

Sean Colloby et al.

Cholinergic muscarinic M1/M4 receptor networks in dementia with Lewy bodies

Anthony Davenport et al.

Advances in therapeutic peptides targeting G protein-coupled receptors

Willem Jespers et al.

X-Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists

Amanda Kennedy, Linda Sundström et al.

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Karol Nass et al.

Advances in long-wavelength native phasing at X-ray free-electron lasers

Alexandra Borodovsky et al.

Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity

Francesca Deflorian et al.

Accurate Prediction of GPCR Ligand Binding Affinity with Free Energy Perturbation

Sarah Bucknell et al.

Structure-Based Drug Discovery of HTL22562: a CGRP Receptor Antagonist For Acute Treatment of Migraine

Miles Congreve et al.

Impact of GPCR Structures on Drug Discovery

Francesca Deflorian et al.

Impact of Recently Determined Crystallographic Structures of GPCRs on Drug Discovery

Mathieu Rappas et al.

Comparison of orexin 1 and orexin 2 ligand binding modes using X-ray crystallography and computational analysis

Rie Suzuki et al.


Nenad Medic et al.

BMI-related cortical morphometry changes are associated with altered white matter structure

Marshall Fiona

Interview with Fiona Marshall

Salas Joaquin J; Martinez-Force Enrique; Venegas-Caleron Monica; Aznar-Moreno Jose Antonio; Garces Rafael; Harwood John L; Moreno-Perez Antonio J; Ruiz-Lopez Noemi; Serrano-Vega Maria J; Graham Ian A; et al

Biochemistry of high stearic sunflower, a new source of saturated fats

Congreve Miles

Meet the editorial board

Hothersall J Daniel; Bussey Charlotte E; Scott James S; Brown Alastair J; Dale Ian; Rawlins Philip

Sustained wash-resistant receptor activation responses of GPR119 agonists

Hothersall J Daniel; Brown Alastair J; Dale Ian; Rawlins Philip

Can residence time offer a useful strategy to target agonist drugs for sustained GPCR responses?

Bergsdorf Christian; Bernet Pascal; Schopfer Ulrich; Ottl Johannes; Duckely Myriam; Fiez-Vandal Cedric; Sykes David A; Charlton Steven J; Aussenac Sonia

An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format

Jones Christopher R; Jones Christopher R; Hatley Oliver J D; Ungell Anna-Lena; Ungell Anna-Lena; Hilgendorf Constanze; Peters Sheila Annie; Rostami-Hodjegan Amin

Gut Wall Metabolism. Application of Pre-Clinical Models for the Prediction of Human Drug Absorption and First-Pass Elimination

Graaf Chris de; Donnelly Dan; Wootten Denise; Lau Jesper; Sexton Patrick M; Miller Laurence J; Ahn Jung-Mo; Liao Jiayu; Fletcher Madeleine M; Yang Dehua; et al

Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes

Soave Mark; Stoddart Leigh A; Woolard Jeanette; Hill Stephen J; Brown Alastair

Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells

Andrews Steve; Congreve Miles

Editorial (Thematic Issue: New Targets for Structure-Based Drug Discovery)

Hatley Oliver J D; Rostami-Hodjegan Amin; Jones Christopher R; Galetin Aleksandra; Rostami-Hodjegan Amin

Quantifying gut wall metabolism: methodology matters

Hatley Oliver J D; Rostami-Hodjegan Amin; Hatley Oliver J D; Galetin Aleksandra; Rostami-Hodjegan Amin; Jones Christopher R

Optimization of intestinal microsomal preparation in the rat: A systematic approach to assess the influence of various methodologies on metabolic activity and scaling factors

Hothersall J Daniel; Torella Rubben; Humphreys Sian; Hooley Monique; McMurray Gordon; Nickolls Sarah A; Brown Alastair

Residues W320 and Y328 within the binding site of the μ-opioid receptor influence opiate ligand bias

Andersen Jacob Lauwring; Lindberg Samsa; Langgard Morten; Maltas Philip J; Ronn Lars Christian Biilmann; Bundgaard Christoffer; Strandbygaard Dorthe; Thirup Soren; Watson Stephen P

The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin

Ayoub Mohammed Akli; Crepieux Pascale; Poupon Anne; Reiter Eric; Ayoub Mohammed Akli; Ayoub Mohammed Akli; Koglin Markus; Parmentier Marc; Parmentier Marc; Pin Jean-Philippe; et al

Antibodies targeting G protein-coupled receptors: Recent advances and therapeutic challenges

Prati Federica; Bottegoni Giovanni; Cavalli Andrea; Bottegoni Giovanni; Bolognesi Maria Laura; Cavalli Andrea

BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease

Horsburgh Karen; Duncombe Jessica; Fowler Jill H; Wardlaw Joanna M; van Agtmael Tom; Harvey Adam; Miller Alyson; Quinn Terry J; Touyz Rhian M; Work Lorraine M; et al

Small vessels, dementia and chronic diseases - molecular mechanisms and pathophysiology

Ellery Jonathan; Dickson Louise; Cheung Toni; Ciuclan Loredana; Bunyard Peter; Mack Stephen; Buffham William J; Farnaby William; Mitchell Philip; Brown Daniel; et al

Identification of compounds acting as negative allosteric modulators of the LPA1 receptor

Monte Didier; Clantin Bernard; Dewitte Frederique; Lens Zoe; Rucktooa Prakash; Verger Alexis; Villeret Vincent; Rucktooa Prakash; Pardon Els; Steyaert Jan; et al

Crystal structure of human Mediator subunit MED23

Tom Ceska et al.

Cryo-EM in drug discovery

Sarah Mancini et al.

On-target and off-target effects of novel orthosteric and allosteric activators of GPR84

Pablo Emiliano Tomatis et al.

Mutations in sigma 70 transcription factor improves expression of functional eukaryotic membrane proteins in Escherichia coli

Amanda Wakefield et al.

Analysis of tractable allosteric sites in G protein-coupled receptors

Tony Warne et al.

Molecular basis for high-affinity agonist binding in GPCRs

Barry O'Neill et al.

The effects of GSK2981710, a medium-chain triglyceride, on cognitive function in healthy older participants: A randomised, placebo-controlled study

Giulio Mattedi et al.

Understanding Ligand Binding Selectivity in a Prototypical GPCR Family

Diamantopoulou, E., et al.

Identification of compounds that rescue otic and myelination defects in the zebrafish adgrg6 (gpr126) mutant

Arimont, M., et al.

Chemokine receptor crystal structures: what can be learnt from them?

Langmead, C.

Determining allosteric modulator mechanism of action: integration of radioligand binding and functional assay data

Mason, J.

Designing multi-target drugs: in vitro panel screening - biological fingerprinting

Cooke, R.

GPCR drug discovery reaches new heights of stability

Mace, O. J., Marshall, F

Digestive Physiology of the Pig Symposium: gut chemosensing and the regulation of nutrient absorption and energy supply

Christopher, J., Congreve, M., Deflorian, F., Marshall, F.

Advances and insights from CNS G protein-coupled receptor crystallography

Erskine. D., et al


Vass. M., et al 

Aminergic GPCR–Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data

Schöppe, J, et al.

Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists

Ehrenmann, J, et al.

High-resolution crystal structure of parathyroid hormone 1 receptor in complex with a peptide agonist

Bortolato, A, Tehan, BG, Smith, RT & Mason, JS

Methodologies for the Examination of Water in GPCRs

Vass, M, et al.

Aminergic GPCR-Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data

Congreve, M, Brown, GA, Borodovsky, A & Lamb, ML

Targeting adenosine A2A receptor antagonism for treatment of cancer

van der Doef, TF, et al.

New approaches in psychiatric drug development.

Brown, DG, et al.

Agonists and Antagonists of Protease-Activated Receptor 2 Discovered within a DNA-Encoded Chemical Library Using Mutational Stabilization of the Target


A2A拮抗薬の 将来性

Christopher, JA, et al.

Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures

Decherchi, S et al.

BiKi Life Sciences: A New Suite for Molecular Dynamics and Related Methods in Drug Discovery

Robertson, N, et al.

Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727.

Rucktooa, P, et al.

Towards high throughput GPCR crystallography: In Meso soaking of Adenosine A2A Receptor crystals.

Jespers, W, et al.

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms.

Soave, M, et al.

A monoclonal antibody raised against a thermo-stabilised β1-adrenoceptor interacts with extracellular loop 2 and acts as a negative allosteric modulator of a sub-set of β1-adrenoceptors expressed in stable cell lines.

Borodovsky, A, et al.

Preclinical pharmacodynamics and antitumor activity of AZD4635, a novel A2A receptor Inhibitor.

Deganutti, G, et al.

Impact of protein–ligand solvation and desolvation on transition state thermodynamic properties of adenosine A2A ligand binding kinetics.

Weinert, T, et al.

Serial millisecond crystallography for routine room-temperature structure determination at synchrotrons.

Congreve, M, Oswald, C & Marshall, FH. 

Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs.

Cheng, RKY, et al.

Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity.

Schuetz, DA, et al.

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time

Hutchings CJ, et al.

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors.

Jazayeri, A, et al.

Crystal structure of the GLP-1 receptor bound to a peptide agonist

Doré, AS, et al.

Decoding Corticotropin-Releasing Factor Receptor Type 1 Crystal Structures.

Cheng, RKY, et al.

Structural insight into allosteric modulation of protease-activated receptor 2.

Congreve, M & Andrews, S.

Perspective in Medicinal Chemistry: Structure-Based Drug Design

Nathan, PJ, et al.

Association between CSF biomarkers, hippocampal volume and cognitive function in patients with amnestic mild cognitive impairment (MCI).

Cooke, RM & Congreve, M.

Allosteric binding: structures reveal new ways to tame G protein-coupled receptors.

Oswald, C, et al.

Intracellular antagonism of the CCR9 receptor.

Congreve, M & Andrews, S.

New Targets for Structure-Based Drug Discovery.

Kuhne, S, et al.

Identification of Ligand Binding Hot Spots of the Histamine H1 Receptor following Structure-Based Fragment Optimization.

Calmet, P, et al.

Real time monitoring of membrane GPCR reconstitution by plasmon waveguide resonance: on the role of lipids.

Lee, S, et al.

How Do Short Chain Nonionic Detergents Destabilize G-Protein-Coupled Receptors?

Marshall, FH.

Visualizing GPCR ‘Megaplexes’ Which Enable Sustained Intracellular Signaling.

Magnani, F, et al

A mutagenesis and screening strategy to generate optimally thermostabilized membrane proteins for structural studies.

Christopher, JA, Doré, AS & Tehan, BG.

Potential for the Rational Design of Allosteric Modulators of Class C GPCRs.

Jazayeri, A, Andrews, SP & Marshall, FH.

Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists.

Tehan, BG & Christopher, JA.

The use of conformationally thermostabilised GPCRs in drug discovery: application to fragment, structure and biophysical techniques.

Segala, E, et al.

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength.

Jazayeri, A, et al..

Extra-helical binding site of a glucagon receptor antagonist.

Congreve, M, & Christopher, JA.

Fragment Screening in Complex Systems.

Weiss, DR, Bortolato, A, Tehan, B & Mason, JS.

GPCR-Bench: A Benchmarking Set and Practitioners’ Guide for G Protein-Coupled Receptor Docking.

Hošek, P, Toulcová, D, Bortolato, A & Spiwok, V.

Altruistic Metadynamics: Multisystem Biased Simulation.

Christopher, JA, Aves, SJ, Bennett, KA, Doré, AS, Errey, JC, Jazayeri, A, Marshall, FH, Okrasa, K, Serrano-Vega, MJ, Tehan, B, Wiggin, GR & Congreve, M.

Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 negative allosteric modulator HTL14242 (3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).

Andrews, SP & Cox, RJ.

Small Molecule CXCR3 Antagonists.

Harpsøe, K, et al.

Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants.

Sato, T, Baker, J, Warne, T, Brown, GA, Leslie, AGW, Congreve, M & Tate, CJ.

Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound β1-Adrenergic Receptor.

Andrews, SP, Aves, SJ, Christopher, JA & Nonoo, R.

Orexin Receptor Antagonists: Historical Perspectives and Future Opportunities.

Bortolato, A, Deflorian, F, Weiss, DR & Mason, JS.

Decoding the Role of Water Dynamics in Ligand-Protein Unbinding: CRF1R as a Test Case.

Mace, O, Tehan, B & Marshall, FH.

Pharmacology and Physiology of Gastrointestinal Enteroendocrine Cells.

Cooke, RM, Brown, AJ, Marshall, FH & Mason, JS.

Structures of G protein-coupled receptors reveal new opportunities for drug discovery.

Kean, J, Bortolato, A, Hollenstein, K, Marshall, FH & Jazayeri, A.

Conformational thermostabilisation of corticotropin releasing factor receptor 1.

Piscitelli, CL, Kean, J, de Graaf, C, Deupi, X.

A Molecular Pharmacologist's Guide to G Protein-Coupled Receptor Crystallography.

Errey, JC, Doré, AS, Zhukov, A, Marshall, FH & Cooke, RM.

Purification of stabilized GPCRs for structural and biophysical analyses.

Jazayeri, A, Dias, JM & Marshall, FH.

From G protein-coupled receptor structure resolution to rational drug design.

Congreve, M & Cooke, R.

Fragment Screening of G Protein-Coupled Receptors

Jazayeri, A & Marshall, F.

Implications of metabotropic glutamate receptor structures for drug discovery in neurotherapeutics.

Christopher, JA, Aves, SJ, Brown, J, Errey, JC, Klair, SS, Langmead, CJ, Mace, OJ, Mould, R, Patel, JC, Tehan, BG, Zhukov, A, Marshall, FH & Congreve, M.

Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties.

Segala, E, Errey, JC, Fiez-Vandal, C, Zhukov, A & Cooke, RM.

Biosensor-based affinities and binding kinetics of small molecule antagonists to the adenosine A2A receptor reconstituted in HDL like particles.

Congreve, M, Doré, AS, Jazayeri, A & Nonoo, R.

Engineering G Protein-Coupled Receptors for Drug Design

He, X, Robertson, N, Jazayeri, A, Gasperina, AG, Schertler, G & Li, X.

Large scale expression and purification of the rat 5-HT2c receptor.

Isberg, V, de Graaf, C, Bortolato, A, Cherezov, V, Katritch, V, Marshall, FH, Mordalski, S, Pin, J-P, Stevens, RC, Vriend, G & Gloriam, DE.

Generic GPCR residue numbers – aligning topology maps while minding the gaps.

Bennett, K, Doré, AS, Christopher, JA, Weiss, DR & Marshall, FH.

Structures of mGluRs shed light on the challenges of drug development of allosteric modulators

Christopher, JA.

Small-molecule antagonists of the orexin receptors.

Koglin, M & Hutchings, CJ.

Targeting G-protein coupled receptors with biologics for therapeutic use – Part 2.

Doré, AS, Okrasa, K, Patel, JC, Serrano-Vega, M, Bennett, K, Cooke, RM, Errey, JC, Jazayeri, A, Khan, S, Tehan, B, Weir, M, Wiggin, GR, & Marshall, FH. 

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

Koglin, M & Hutchings, CJ.

Targeting G-protein coupled receptors with biologics for therapeutic use – Part 1.

Bortolato, A, Doré, AS, Hollenstein, K, Mason, JS & Marshall, FH.

Structure of Class B GPCRs: new horizons for drug discovery.

Tehan, BG, Bortolato, A, Blaney, FE, Weir, MP & Mason, JS.

Unifying Family A GPCR Theories of Activation.

Andrews, SP, Brown, GA & Christopher, JA.

Structure-based and fragment-based GPCR drug discovery.

Hollenstein, K, de Graaf, C, Bortolato, A, Wang, M-W, Marshall, FH & Stevens, RC.

Insights into the structure of class B GPCRs.

Congreve, M, Dias, JM & Marshall, FH.

Structure-based drug design for G protein-coupled receptors.

Andrews, SP, Mason, JS, Hurrell, E & Congreve, M.

Structure-based drug design of chromone antagonists of the adenosine A2A receptor.

Hutchings, CJ, Cseke, G, Osborne, G, Woolard, J, Zhukov, A, Koglin, M, Jazayeri, A, Pandya-Pathak, J, Langmead, CJ, Hill, S, Weir, M & Marshall, FH.

Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment.

Mould, R, Brown, J, Marshall, FH & Langmead, CJ.

Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands.

Mason, JS, Bortolato, A, Weiss, DR, Deflorian, F, Tehan, B & Marshall, FH.

High end GPCR design: crafted ligand design and druggability analysis using protein structure, lipophilic hotspots and explicit water networks.

Bortolato, A, Tehan, BG, Bodnarchuk, MS, Essex, JW & Mason, JS.

Water network perturbation in ligand binding: Adenosine A2A antagonists as a case study.

Hollenstein, K, Kean, J, Bortolato, A, Cheng, RKY, Doré, AS, Jazayeri, A, Cooke, RM, Weir, MP & Marshall, FH.

Structure of class B GPCR corticotropin-releasing factor receptor 1.

Christopher, JA, Brown, J, Doré, AS, Errey, JC, Koglin, M, Marshall, FH, Myszka, DG, Rich, RL, Tate, CG, Tehan, B, Warne, T & Congreve, M.

Biophysical fragment screening of the β1 adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.

Bennett, KA, Tehan, B, Lebon, G, Tate, CG, Weir, MP, Marshall, FH & Langmead, CJ.

Pharmacology and structure of isolated conformations of the adenosine A2A receptor define ligand efficacy.

Cooke, RM, Koglin, M, Errey, JC & Marshall, FH.

Preparation of purified GPCRs for structural studies.

Christopher, JA & Congreve, M.

Treatment and prevention of various therapeutic conditions using OX receptor antagonistic activity. (WO2012081692).

Andrews, S. P. and Tehan, B.

Stabilised G protein-coupled receptors in structure-based drug design: a case study with adenosine A2A receptor

Christopher, JA.

Orexin receptor antagonists: a review of the patent literature 2009-2011.

Chen, D, Errey, JC, Heitman, LH, Marshall, FH, IJzerman, AP & Siegal, G.

Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A2A Receptor with novel biological activity

Owen, RL, Axford, D, Nettleship, JE, Owens, RJ, Robinson, JI, Morgan, AW, Doré, AS, Lebon, G, Tate, CG, Fry, EE, Ren, J, Stuart, DI & Evans G.

Outrunning free radicals in room-temperature macromolecular crystallography. Acta Cryst. D. 2012, 68: 810-818.

Mason, JS, Bortolato, A, Congreve, M & Marshall, FH.

New insights from structural biology into the druggability of G protein-coupled receptors

Congreve, M, Langmead, C & Marshall, FH.

The use of GPCR structures in drug design.

Langmead, CJ, Andrews, SP, Congreve, M, Errey, JC, Hurrell, E, Marshall, FH, Mason, JS, Richardson, CM, Robertson, N, Zhukov, A & Weir, MP.

Identification of novel adenosine A2A receptor antagonists by virtual screening

Congreve, M, Andrews, SP, Doré, AS, Errey, JC, Hollenstein, K, Hurrell, E, Langmead, CJ, Mason, JS, Ng, IW, Tehan, B, Zhukov, A, Weir, MP & Marshall, FH.

Discovery of 1,2,4-triazine derivatives as adenosine A2A antagonists using structure based drug design

Doré, AS, Robertson, N, Errey, JC, Ng, I, Hollenstein, K, Tehan, B, Hurrell, E, Bennett, K, Congreve, M, Magnani, F, Tate, CG, Weir, MP & Marshall, FH.

Structure of the adenosine A2A receptor in complex with ZM241385 and the xanthines XAC and caffeine

Zhukov, A, Andrews, SP, Errey, JC, Robertson, N, Tehan, B, Mason, JS, Marshall, FH, Weir, MP & Congreve, M.

Biophysical mapping of adenosine A2A receptor.

Congreve, M, Langmead, CJ, Mason, JS & Marshall, FH

Progress in structure based drug design for G protein-coupled receptors.

Rich, RL, Errey, J, Marshall, F & Myszka, DG.

Biacore analysis with stabilized G-protein-coupled receptors.

Lebon, G, Warne, T, Edwards, PC, Bennett, K, Langmead, CJ, Leslie, AGW & Tate, CG.

Agonist-bound structures of the adenosine A2A reveals common features of GPCR activation.

Congreve, M, Rich, RL, Myszka, DG, Figaroa, F, Siegal, G & Marshall, FH.

Fragment screening of stabilized G-protein-coupled receptors using biophysical methods.

Lebon, G, Bennett, K, Jazayeri, A & Tate, CG.

Thermostabilisation of an agonist-bound conformation of the human adenosine A2A receptor.

Robertson, N, Jazayeri, A, Errey, J, Baig, A, Hurrell, E, Zhukov, A, Langmead, CJ, Weir, MP & Marshall, FH.

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

Hutchings CJ, Koglin M, and Marshall FH.

Therapeutic antibodies directed at G-protein-coupled receptors.

Marshall FH and Foord SM.

Heterodimerization of the GABAB receptor-implications for GPCR signaling and drug discovery.

Errey, JC & Marshall, FH.

New techniques to express and crystallise G-protein coupled receptors

Congreve, M & Marshall F.

The impact of GPCR structures on pharmacology and structure- based drug design.

Congreve, M, Bortolato, A, Brown, G & Cooke, RM.

Modeling and Design for Membrane Protein Targets.