M. Congreve

发表

Structural biology and drug discovery.

T. Blundell, M. Congreve, C. Murray, 2005, Drug discovery today.

Recent developments in fragment-based drug discovery.

M. Congreve, G. Chessari, A. Woodhead, 2008, Journal of medicinal chemistry.

A 'rule of three' for fragment-based lead discovery?

M. Congreve, C. Murray, H. Jhoti, 2003, Drug discovery today.

Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine.

M. Congreve, A. Doré, J. Errey, 2011, Structure.

Keynote review: Structural biology and drug discovery

Tom L. Blundell, Miles Congreve, Christopher W. Murray, 2005 .

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).

Ali Jazayeri, Benjamin G. Tehan, Miles Congreve, 2015, Journal of medicinal chemistry.

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.

M. Congreve, J. Mason, A. Doré, 2018, Journal of medicinal chemistry.

Fragment-based lead discovery: leads by design.

Christopher W Murray, Miles Congreve, M. Congreve, 2005, Drug discovery today.

Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency.

Gianni Chessari, Brent Graham, Christopher W Murray, 2010, Journal of medicinal chemistry.

Solid-phase reaction monitoring--chemical derivatization and off-bead analysis.

M. Congreve, S. Ley, N. Parr, 2000, Biotechnology and bioengineering.

Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase.

Gianni Chessari, Christopher W Murray, Miles Congreve, 2007, Journal of medicinal chemistry.

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

J. Mellor, M. Congreve, Jon Palacios-Filardo, 2020, Nature Communications.

Progress in Structure Based Drug Design for G Protein-Coupled Receptors

Jonathan S. Mason, Christopher J. Langmead, Miles Congreve, 2011, Journal of medicinal chemistry.

Fragment Screening in Complex Systems

M. Congreve, J. Christopher, 2016 .

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

Gregg Siegal, Rebecca L Rich, David G Myszka, 2011, Methods in enzymology.

THEMED SECTION: MOLECULAR PHARMACOLOGY OF G PROTEIN-COUPLED RECEPTORS REVIEW The impact of GPCR structures on pharmacology and structure-based drug design

M. Congreve, F. Marshall, 2010 .

Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.

Christopher W Murray, Alessandro Padova, Jayne Curry, 2005, Journal of medicinal chemistry.

Application of fragment screening and fragment linking to the discovery of novel thrombin inhibitors.

Gianni Chessari, Chris Abell, Christopher W Murray, 2006, Journal of medicinal chemistry.

Modeling and Design for Membrane Protein Targets

M. Congreve, A. Bortolato, R. Cooke, 2017 .

A novel phase-switching protecting group for multi-step parallel solution phase synthesis.

M. Congreve, C. Abell, M. Ladlow, 2004, Organic & biomolecular chemistry.

Impact of GPCR Structures on Drug Discovery

M. Congreve, C. Tate, C. Graaf, 2020, Cell.

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

M. Congreve, C. Langmead, J. Errey, 2015 .

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

M. Congreve, J. Mason, J. Åqvist, 2020, Angewandte Chemie.

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

James D. Clarke, M. Congreve, B. Linghu, 2020, Journal for ImmunoTherapy of Cancer.

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

M. Congreve, J. Mason, J. Åqvist, 2019, Angewandte Chemie.

Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M 1 -acetylcholine receptor agonist: A randomized cross-over trial

M. Congreve, F. Marshall, P. Nathan, 2021 .

Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.

M. Congreve, J. Mason, A. Doré, 2020 .

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

S. P. Andrews, M. Congreve, J. Mason, 2014 .

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

M. Congreve, J. Christopher, 2013, Expert opinion on therapeutic patents.

Intracellular allosteric antagonism of the CCR9 receptor

Ali Jazayeri, Jonathan S. Mason, Francesca Deflorian, 2016, Nature.

Ascidiatrienolide A is a 10-membered lactone

M. Congreve, A. Holmes, M. Looney, 1993 .

Ascidiatrienolide A is a 10-Membered Lactone.

M. Congreve, A. Holmes, M. Looney, 1993 .

Biophysical Fragment Screening of the β1-Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

Christopher G. Tate, David G. Myszka, Miles Congreve, 2013, Journal of medicinal chemistry.

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

Andrea Bortolato, Miles Congreve, Jonathan S Mason, 2012, Trends in pharmacological sciences.

Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug Design

Jonathan S. Mason, Christopher J. Langmead, S. P. Andrews, 2012, Journal of medicinal chemistry.

Versatile solid-phase synthesis of secondary amines from alcohols. Development of an N-Boc-(o-nitrobenzene)sulfonamide linker

M. Congreve, S. Ley, J. Scicinski, 2003 .

Reporter resins for solid-phase chemistry.

M. Congreve, M. Ladlow, T. Sheppard, 2001, Organic letters.

A Rapid Approach for the Optimisation of Polymer Supported Reagents in Synthesis

Steven V. Ley, M. Congreve, S. Ley, 2000 .

Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.

Gianni Chessari, Mark Sylvester, Rutger H A Folmer, 2007, Journal of medicinal chemistry.

Synthesis of 5-N-Substituted Tetrazole Derivatives of the Potent NK1 Receptor Antagonist GR203040

M. Congreve, 1996 .

Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound

M. Congreve, P. Ward, S. Watson, 1996 .

Application of fragment screening by X-ray crystallography to beta-secretase.

Gianni Chessari, Christopher W Murray, Miles Congreve, 2007, Journal of medicinal chemistry.

High-throughput analytical techniques for reaction optimization.

M. Congreve, C. Jamieson, Miles S Congreve, 2002, Drug discovery today.

2‐Ethyl‐7‐hydroxybenzisoxazolium Tetrafluoroborate

M. Congreve, 2001 .

Application of ReactArray Robotics and Design of Experiments Techniques in Optimisation of Supported Reagent Chemistry

Steven V. Ley, Miles Congreve, M. Congreve, 2002 .

Oxidation state of the active-site cysteine in protein tyrosine phosphatase 1B

Miles Congreve, M. Congreve, H. Jhoti, 2003, Nature.

Synthesis of (+)-obtusenyne.

M. Congreve, J. Davies, A. Holmes, 2008, Chemistry.

Detection of ligands from a dynamic combinatorial library by X-ray crystallography.

Paul G Wyatt, M. Congreve, H. Jhoti, 2003, Angewandte Chemie.

Biophysical Mapping of the Adenosine A2A Receptor

Nathan Robertson, Jonathan S. Mason, S. P. Andrews, 2011, Journal of medicinal chemistry.

Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.

Gianni Chessari, Brent Graham, Jose Cosme, 2010, Journal of medicinal chemistry.

1,4-Benzodiazepin-2-one derived neurokinin-1 receptor antagonists

M. Congreve, P. Ward, A. B. Hawcock, 1997 .

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

Miles Congreve, Fiona Marshall, M. Congreve, 2010, British journal of pharmacology.

Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.

Paul N. Mortenson, M. Congreve, R. Cheng, 2012, ACS medicinal chemistry letters.

Targeting adenosine A2A receptor antagonism for treatment of cancer

Michelle L. Lamb, Miles Congreve, M. Congreve, 2018, Expert opinion on drug discovery.

Article pubs.acs.org/jmc Identification of Novel Adenosine A 2A Receptor Antagonists by Virtual Screening

Nathan Robertson, Jonathan S. Mason, Christopher J. Langmead, 2022 .

Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.

Gianni Chessari, Mladen Vinković, Miles Congreve, 2008, Journal of medicinal chemistry.

Recent Developments in Fragment-Based Drug Discovery

M. Congreve, G. Chessari, A. Woodhead, 2008 .

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

M. Congreve, F. Marshall, P. Nathan, 2020, British journal of clinical pharmacology.

Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors.

M. Congreve, J. Christopher, Giles A. Brown, 2020, Journal of medicinal chemistry.

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

M. Congreve, F. Marshall, P. Nathan, 2021, British journal of clinical pharmacology.

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

M. Congreve, F. Marshall, P. Nathan, 2021, Alzheimer's research & therapy.

Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): a Calcitonin Gene-Related Pepti

M. Congreve, J. Mason, F. Deflorian, 2020, Journal of medicinal chemistry.

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

Ali Jazayeri, Jonathan S. Mason, Andrea Bortolato, 2017, Nature.

The use of GPCR structures in drug design.

Miles Congreve, Fiona H Marshall, Christopher Langmead, 2011, Advances in pharmacology.

Chapter 28 Fragment-Based Lead Discovery

Miles Stuart Congreve, Christopher W. Murray, Robin Arthur Ellis Carr, 2007 .

Structure‐Based Drug Design for G Protein‐Coupled Receptors

M. Congreve, C. Graaf, J. Christopher, 2021 .

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

M. Congreve, J. Mason, J. Åqvist, 2019, Angewandte Chemie.

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

M. Congreve, P. Maruff, P. Nathan, 2022, Alzheimer's & dementia.

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

Jillian Baker, Christopher G Tate, Miles Congreve, 2015, Molecular Pharmacology.

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

M. Congreve, F. Marshall, C. Oswald, 2017, Trends in pharmacological sciences.

Searching for Chemokine Receptor Binding Antagonists by High Throughput Screening

M. Congreve, M. Banks, G. Mellor, 1997 .

Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis

M. Congreve, J. Mason, J. Errey, 2019, Journal of medicinal chemistry.

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

S. P. Andrews, M. Congreve, J. Mason, 2017, Nature.

Accurate Prediction of GPCR Ligand Binding Affinity with Free Energy Perturbation

Chris de Graaf, Herman van Vlijmen, Jonathan S. Mason, 2020, J. Chem. Inf. Model..

Ask the experts: past, present and future of the rule of five.

M. Congreve, P. Leeson, J. Baell, 2013, Future medicinal chemistry.

From structure to clinic: Design of a muscarinic M1 receptor agonist with the potential to treat Alzheimer’s disease

Stephen R. Morairty, Robert T. Smith, G. Dawson, 2021, Cell.

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

Miles Congreve, Fiona H Marshall, M. Congreve, 2014, Progress in medicinal chemistry.

Engineering G Protein-Coupled Receptors for Drug Design

M. Congreve, A. Jazayeri, A. S. Doré, 2015 .

Development of an indole safety-catch linker using analytical constructs.

M. Congreve, S. Ley, J. Scicinski, 2004, Journal of combinatorial chemistry.

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

M. Congreve, R. Cooke, 2016, Future medicinal chemistry.

Fragment-Based Screening by X-ray Crystallography

Miles Stuart Congreve, I. J. Tickle, Valerio Berdini, 2007 .

Crystal Structure of Human Soluble Adenylate Cyclase Reveals a Distinct, Highly Flexible Allosteric Bicarbonate Binding Pocket

M. Congreve, C. Murray, V. Berdini, 2014, ChemMedChem.

Fragment-based lead discovery

M. Congreve, C. Murray, D. Rees, 2004, Nature Reviews Drug Discovery.

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

J. Mellor, M. Congreve, Jon Palacios-Filardo, 2021, Nature Communications.

TEMPORARY REMOVAL: Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design.

S. P. Andrews, M. Congreve, J. Mason, 2019, Bioorganic & medicinal chemistry letters.

Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.

M. Congreve, J. Mason, A. Bortolato, 2022, ACS chemical neuroscience.

Abstract 5580: Preclinical pharmacodynamics and antitumor activity of AZD4635, a novel adenosine 2A receptor inhibitor that reverses adenosine mediated T cell suppression

James D. Clarke, M. Congreve, J. Mason, 2017 .

Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency.

M. Congreve, C. Murray, G. Chessari, 2010, Journal of medicinal chemistry.

A Rapid Approach for the Optimisation of Polymer Supported Reagents in Synthesis

M. Congreve, S. Ley, C. Jamieson, 2000 .

Synthesis of (+)-obtusenyne.

M. Congreve, J. Davies, A. Holmes, 2008, Chemistry.

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

A. Leslie, Tomomi Sato, M. Congreve, 2015, Molecular Pharmacology.

Faculty Opinions recommendation of Dual catalysis. Merging photoredox with nickel catalysis: coupling of α-carboxyl sp³-carbons with aryl halides.

M. Congreve, M. Pickworth, 2014 .