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

por Congreve, Miles, Langmead, Christopher J., Mason, Jonathan S., Marshall, Fiona H.
Publicado 2011

Biophysical Mapping of the Adenosine A(2A) Receptor

por Zhukov, Andrei, Andrews, Stephen P., Errey, James C., Robertson, Nathan, Tehan, Benjamin, Mason, Jonathan S., Marshall, Fiona H., Weir, Malcolm, Congreve, Miles
Publicado 2011

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

por Palacios-Filardo, Jon, Udakis, Matt, Brown, Giles A., Tehan, Benjamin G., Congreve, Miles S., Nathan, Pradeep J., Brown, Alastair J. H., Mellor, Jack R.
Publicado 2021

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

por Palacios-Filardo, Jon, Udakis, Matt, Brown, Giles A., Tehan, Benjamin G., Congreve, Miles S., Nathan, Pradeep J., Brown, Alastair J. H., Mellor, Jack R.
Publicado 2021

Identification of Novel Adenosine A(2A) Receptor Antagonists by Virtual Screening

por Langmead, Christopher J., Andrews, Stephen P., Congreve, Miles, Errey, James C., Hurrell, Edward, Marshall, Fiona H., Mason, Jonathan S., Richardson, Christine M., Robertson, Nathan, Zhukov, Andrei, Weir, Malcolm
Publicado 2012

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

por Congreve, Miles, Andrews, Stephen P., Doré, Andrew S., Hollenstein, Kaspar, Hurrell, Edward, Langmead, Christopher J., Mason, Jonathan S., Ng, Irene W., Tehan, Benjamin, Zhukov, Andrei, Weir, Malcolm, Marshall, Fiona H.
Publicado 2012

Biophysical Fragment Screening of the β(1)-Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

por Christopher, John A., Brown, Jason, Doré, Andrew S., Errey, James C., Koglin, Markus, Marshall, Fiona H., Myszka, David G., Rich, Rebecca L., Tate, Christopher G., Tehan, Benjamin, Warne, Tony, Congreve, Miles
Publicado 2013

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

por Saalau-Bethell, Susanne M, Berdini, Valerio, Cleasby, Anne, Congreve, Miles, Coyle, Joseph E, Lock, Victoria, Murray, Christopher W, O'Brien, M Alistair, Rich, Sharna J, Sambrook, Tracey, Vinkovic, Mladen, Yon, Jeff R, Jhoti, Harren
Publicado 2014

Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M(1) receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending...

por Bakker, Charlotte, Tasker, Tim, Liptrot, Jan, Hart, Ellen P., Klaassen, Erica S., Doll, Robert Jan, Brown, Giles A., Brown, Alastair, Congreve, Miles, Weir, Malcolm, Marshall, Fiona H., Cross, David M., Groeneveld, Geert Jan, Nathan, Pradeep J.
Publicado 2021

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

por Bakker, Charlotte, Prins, Samantha, Liptrot, Jan, Hart, Ellen P., Klaassen, Erica S., Brown, Giles A., Brown, Alastair, Congreve, Miles, Weir, Malcolm, Marshall, Fiona H., Stevens, Jasper, Cross, David M., Tasker, Tim, Nathan, Pradeep J., Groeneveld, Geert Jan
Publicado 2021

X‐Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A(2A) Adenosine Receptor Antagonists

por Jespers, Willem, Verdon, Grégory, Azuaje, Jhonny, Majellaro, Maria, Keränen, Henrik, García‐Mera, Xerardo, Congreve, Miles, Deflorian, Francesca, de Graaf, Chris, Zhukov, Andrei, Doré, Andrew S., Mason, Jonathan S., Åqvist, Johan, Cooke, Robert M., Sotelo, Eddy, Gutiérrez‐de‐Terán, Hugo
Publicado 2020

A phase 1b/2a multicenter study of the safety and preliminary pharmacodynamic effects of selective muscarinic M(1) receptor agonist HTL0018318 in patients with mild‐to‐moderate Alz...

por Nathan, Pradeep J., Millais, S. Babli, Godwood, Alex, Dewit, Odile, Cross, David M., Liptrot, Janet, Ruparelia, Bharat, Jones, Stephen Paul, Bakker, Geor, Maruff, Paul T., Light, Gregory A., Brown, Alastair J.H., Weir, Malcolm Peter, Congreve, Miles, Tasker, Tim
Publicado 2022

First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M(1)‐receptor partial agonist for the treatment of dementias...

por Bakker, Charlotte, Tasker, Tim, Liptrot, Jan, Hart, Ellen P., Klaassen, Erica S., Prins, Samantha, van der Doef, Thalia F., Brown, Giles A., Brown, Alastair, Congreve, Miles, Weir, Malcolm, Marshall, Fiona H., Cross, David M., Groeneveld, Geert Jan, Nathan, Pradeep J.
Publicado 2021

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

por Rappas, Mathieu, Ali, Ammar A. E., Bennett, Kirstie A., Brown, Jason D., Bucknell, Sarah J., Congreve, Miles, Cooke, Robert M., Cseke, Gabriella, de Graaf, Chris, Doré, Andrew S., Errey, James C., Jazayeri, Ali, Marshall, Fiona H., Mason, Jonathan S., Mould, Richard, Patel, Jayesh C., Tehan, Benjamin G., Weir, Malcolm, Christopher, John A.
Publicado 2019

Small molecule AZD4635 inhibitor of A(2A)R signaling rescues immune cell function including CD103(+) dendritic cells enhancing anti-tumor immunity

por Borodovsky, Alexandra, Barbon, Christine M, Wang, Yanjun, Ye, Minwei, Prickett, Laura, Chandra, Dinesh, Shaw, Joseph, Deng, Nanhua, Sachsenmeier, Kris, Clarke, James D, Linghu, Bolan, Brown, Giles A, Brown, James, Congreve, Miles, Cheng, Robert KY, Dore, Andrew S, Hurrell, Edward, Shao, Wenlin, Woessner, Richard, Reimer, Corinne, Drew, Lisa, Fawell, Stephen, Schuller, Alwin G, Mele, Deanna A
Publicado 2020