Impact of GPCR Structures on Drug Discovery von Congreve, Miles, de Graaf, Chris, Swain, Nigel A., Tate, Christopher G.

Volltext

Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs von Congreve, Miles, Oswald, Christine, Marshall, Fiona H.

Volltext

The impact of GPCR structures on pharmacology and structure‐based drug design von Congreve, Miles, Marshall, Fiona

Volltext

Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits von Palacios-Filardo, Jon, Udakis, Matt, Brown, Giles A., Tehan, Benjamin G., Congreve, Miles S., Nathan, Pradeep J., Brown, Alastair J. H., Mellor, Jack R.

Volltext

A ‘Rule of Three’ for fragment-based lead discovery? von Congreve, Miles, Carr, Robin, Murray, Chris, Jhoti, Harren

Volltext

Progress in Structure Based Drug Design for G Protein-Coupled Receptors von Congreve, Miles, Langmead, Christopher J, Mason, Jonathan S, Marshall, Fiona H

Volltext

Crystal structure of the GLP-1 receptor bound to a peptide agonist von Jazayeri, Ali, Rappas, Mathieu, Brown, Alastair J. H., Kean, James, Errey, James C., Robertson, Nathan J., Fiez-Vandal, Cédric, Andrews, Stephen P., Congreve, Miles, Bortolato, Andrea, Mason, Jonathan S., Baig, Asma H., Teobald, Iryna, Doré, Andrew S., Weir, Malcolm, Cooke, Robert M., Marshall, Fiona H.

Volltext

From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease von Brown, Alastair J H, Bradley, Sophie J, Marshall, Fiona H, Brown, Giles A, Bennett, Kirstie A, Brown, Jason, Cansfield, Julie E, Cross, David M, de Graaf, Chris, Hudson, Brian D, Dwomoh, Louis, Dias, João M, Errey, James C, Hurrell, Edward, Liptrot, Jan, Mattedi, Giulio, Molloy, Colin, Nathan, Pradeep J, Okrasa, Krzysztof, Osborne, Greg, Patel, Jayesh C, Pickworth, Mark, Robertson, Nathan, Shahabi, Shahram, Bundgaard, Christoffer, Phillips, Keith, Broad, Lisa M, Goonawardena, Anushka V, Morairty, Stephen R, Browning, Michael, Perini, Francesca, Dawson, Gerard R, Deakin, John F W, Smith, Robert T, Sexton, Patrick M, Warneck, Julie, Vinson, Mary, Tasker, Tim, Tehan, Benjamin G, Teobald, Barry, Christopoulos, Arthur, Langmead, Christopher J, Jazayeri, Ali, Cooke, Robert M, Rucktooa, Prakash, Congreve, Miles S, Weir, Malcolm, Tobin, Andrew B

Volltext

Fragment-based lead discovery von Rees, David C, Congreve, Miles, Murray, Christopher W, Carr, Robin

Volltext

Author Correction: Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits von Palacios-Filardo, Jon, Udakis, Matt, Brown, Giles A., Tehan, Benjamin G., Congreve, Miles S., Nathan, Pradeep J., Brown, Alastair J. H., Mellor, Jack R.

Volltext

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

Volltext

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

Volltext

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]be... von Christopher, John A, Aves, Sarah J, Bennett, Kirstie A, Doré, Andrew S, Errey, James C, Jazayeri, Ali, Marshall, Fiona H, Okrasa, Krzysztof, Serrano-Vega, Maria J, Tehan, Benjamin G, Wiggin, Giselle R, Congreve, Miles

Volltext

Fragment Screening of Stabilized G-Protein-Coupled Receptors Using Biophysical Methods von Congreve, Miles, Rich, Rebecca L., Myszka, David G., Figaroa, Francis, Siegal, Gregg, Marshall, Fiona H.

Volltext

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... von Woodhead, Andrew J, Angove, Hayley, Carr, Maria G, Chessari, Gianni, Congreve, Miles, Coyle, Joseph E, Cosme, Jose, Graham, Brent, Day, Philip J, Downham, Robert, Fazal, Lynsey, Feltell, Ruth, Figueroa, Eva, Frederickson, Martyn, Lewis, Jonathan, McMenamin, Rachel, Murray, Christopher W, O’Brien, M. Alistair, Parra, Lina, Patel, Sahil, Phillips, Theresa, Rees, David C, Rich, Sharna, Smith, Donna-Michelle, Trewartha, Gary, Vinkovic, Mladen, Williams, Brian, Woolford, Alison J.-A

Volltext

Oxidation state of the active-site cysteine in protein tyrosine phosphatase 1B von Jhoti, Harren, van Montfort, Rob L. M, Congreve, Miles, Tisi, Dominic, Carr, Robin

Volltext

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

Volltext

Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode von Southall, Stacey M., Banerjee, Joydeep, Brown, Jason, Butkovic, Kristina, Cansfield, Andrew D., Cansfield, Julie E., Congreve, Miles S., Cseke, Gabriella, Deflorian, Francesca, Hunjadi, Martina Petrovic, Hutinec, Antun, Inturi, Trinadh Kumar, Rupcic, Renata, Saxty, Gordon, Watson, Stephen P.

Volltext

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

Volltext

Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation von Gill, Adrian L, Frederickson, Martyn, Cleasby, Anne, Woodhead, Steven J, Carr, Maria G, Woodhead, Andrew J, Walker, Margaret T, Congreve, Miles S, Devine, Lindsay A, Tisi, Dominic, O'Reilly, Marc, Seavers, Lisa C. A, Davis, Deborah J, Curry, Jayne, Anthony, Rachel, Padova, Alessandro, Murray, Christopher W, Carr, Robin A. E, Jhoti, Harren

Volltext