Search Results - "Brown, Giles A."

Towards high throughput GPCR crystallography: In Meso soaking of Adenosine A2A Receptor crystals by Rucktooa, Prakash, Cheng, Robert K. Y., Segala, Elena, Geng, Tian, Errey, James C., Brown, Giles A., Cooke, Robert M., Marshall, Fiona H., Doré, Andrew S.

“…Here we report an efficient method to generate multiple co-structures of the A 2A G protein-coupled receptor (GPCR) with small-molecules from a single…”
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Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits by Palacios-Filardo, Jon, Udakis, Matt, Brown, Giles A., Tehan, Benjamin G., Congreve, Miles S., Nathan, Pradeep J., Brown, Alastair J. H., Mellor, Jack R.

“…Acetylcholine release in the hippocampus plays a central role in the formation of new memory representations. An influential but largely untested theory…”
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Structure-Based and Fragment-Based GPCR Drug Discovery by Andrews, Stephen P., Brown, Giles A., Christopher, John A.

“…G protein‐coupled receptors (GPCRs) are an important family of membrane proteins; historically, drug discovery in this target class has been fruitful, with…”
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Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity by Borodovsky, Alexandra, Barbon, Christine M, Wang, Yanjun, Ye, Minwei, Prickett, Laura, Chandra, Dinesh, Shaw, Joseph, Deng, Nanhua, Sachsenmeier, Kris, Clarke, James D, Bolan Linghu, 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

“…Accumulation of extracellular adenosine within the microenvironment is a strategy exploited by tumors to escape detection by the immune system. Adenosine…”
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Author Correction: Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits by Palacios-Filardo, Jon, Udakis, Matt, Brown, Giles A., Tehan, Benjamin G., Congreve, Miles S., Nathan, Pradeep J., Brown, Alastair J. H., Mellor, Jack R.

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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 by 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.

“…Abstract Background The cholinergic system and M 1 receptor remain an important target for symptomatic treatment of cognitive dysfunction. The selective M 1…”
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Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors by Suzuki, Rie, Brown, Giles A, Christopher, John A, Scully, Conor C. G, Congreve, Miles

“…Glucagon-like peptide 1 (GLP-1) and glucagon-like peptide 2 (GLP-2) are proglucagon derived peptides that are released from gut endocrine cells in response to…”
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Structural insight into allosteric modulation of protease-activated receptor 2 by Cheng, Robert K. Y., Fiez-Vandal, Cédric, Schlenker, Oliver, Edman, Karl, Aggeler, Birte, Brown, Dean G., Brown, Giles A., Cooke, Robert M., Dumelin, Christoph E., Doré, Andrew S., Geschwindner, Stefan, Grebner, Christoph, Hermansson, Nils-Olov, Jazayeri, Ali, Johansson, Patrik, Leong, Louis, Prihandoko, Rudi, Rappas, Mathieu, Soutter, Holly, Snijder, Arjan, Sundström, Linda, Tehan, Benjamin, Thornton, Peter, Troast, Dawn, Wiggin, Giselle, Zhukov, Andrei, Marshall, Fiona H., Dekker, Niek

“…Crystal structures of protease-activated receptor 2 (PAR2) in complex with two different antagonist ligands and with a blocking antibody reveal binding sites…”
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From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease by 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

“…Current therapies for Alzheimer's disease seek to correct for defective cholinergic transmission by preventing the breakdown of acetylcholine through…”
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Targeting adenosine A 2A receptor antagonism for treatment of cancer by Congreve, Miles, Brown, Giles A, Borodovsky, Alexandra, Lamb, Michelle L

“…Adenosine A Receptor (A R) antagonists are an emerging class of agents that treat cancers, both as a monotherapy and in combination with other therapeutic…”
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Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound β1-Adrenergic Receptor by Sato, Tomomi, Baker, Jillian, Warne, Tony, Brown, Giles A, Leslie, Andrew G W, Congreve, Miles, Tate, Christopher G

“…Comparisons between structures of the β1-adrenergic receptor (AR) bound to either agonists, partial agonists, or weak partial agonists led to the proposal that…”
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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 by 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

“…HTL0018318 is a selective M receptor partial agonist currently under development for the symptomatic treatment of cognitive and behavioural symptoms in…”
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First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1‐receptor partial agonist for the treatment of dementias by Bakker, Charlotte, Tasker, Tim, Liptrot, Jan, Hart, Ellen P., Klaassen, Erica S., Prins, Samantha, Doef, Thalia F., Brown, Giles A., Brown, Alastair, Congreve, Miles, Weir, Malcolm, Marshall, Fiona H., Cross, David M., Groeneveld, Geert Jan, Nathan, Pradeep J.

“…Aims HTL0018318 is a selective M1 receptor partial agonist currently under development for the symptomatic treatment of cognitive and behavioural symptoms in…”
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Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M1‐acetylcholine receptor agonist: A randomized cross‐over trial by 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

“…Aims HTL0009936 is a selective M1 muscarinic receptor agonist in development for cognitive dysfunction in Alzheimer's disease. Safety, tolerability and…”
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Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M 1 -acetylcholine receptor agonist: A randomized cross-over trial by 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

“…HTL0009936 is a selective M muscarinic receptor agonist in development for cognitive dysfunction in Alzheimer's disease. Safety, tolerability and…”
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Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein–Ligand Complexes by Cansfield, Andrew D, Ator, Mark A, Banerjee, Joydeep, Bestwick, Michael, Bortolato, Andrea, Brown, Giles A, Brown, Jason, Butkovic, Kristina, Cansfield, Julie E, Christopher, John A, Congreve, Miles, Cseke, Gabriella, Deflorian, Francesca, Dugan, Benjamin, Hunjadi, Martina Petrovic, Hutinec, Antun, Inturi, Trinadh Kumar, Landek, Goran, Mason, Jonathan, O’Brien, Alistair, Ott, Gregory R, Rupcic, Renata, Saxty, Gordon, Southall, Stacey M, Zadravec, Rahela, Watson, Stephen P

“…A series of macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonists identified using structure-based design principles, exemplified by…”
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Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure-based drug design by O'Brien, Alistair, Andrews, Stephen P., Baig, Asma H., Bortolato, Andrea, Brown, Alastair J.H., Brown, Giles A., Brown, Sue H., Christopher, John A., Congreve, Miles, Cooke, Robert M., De Graaf, Chris, Errey, James C., Fieldhouse, Charlotte, Jazayeri, Ali, Marshall, Fiona H., Mason, Jonathan S., Mobarec, Juan Carlos, Okrasa, Krzysztof, Steele, Kelly N., Southall, Stacey M., Teobald, Iryna, Watson, Steve P., Weir, Malcolm

“…A series of novel allosteric antagonists of the GLP-1 receptor (GLP-1R), exemplified by HTL26119, are described. [Display omitted] A series of novel allosteric…”
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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 dose study by 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

“…The cholinergic system and M receptor remain an important target for symptomatic treatment of cognitive dysfunction. The selective M receptor partial agonist…”
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Agonists and Antagonists of Protease-Activated Receptor 2 Discovered within a DNA-Encoded Chemical Library Using Mutational Stabilization of the Target by Brown, Dean G, Brown, Giles A, Centrella, Paolo, Certel, Kaan, Cooke, Robert M, Cuozzo, John W, Dekker, Niek, Dumelin, Christoph E, Ferguson, Andrew, Fiez-Vandal, Cédric, Geschwindner, Stefan, Guié, Marie-Aude, Habeshian, Sevan, Keefe, Anthony D, Schlenker, Oliver, Sigel, Eric A, Snijder, Arjan, Soutter, Holly T, Sundström, Linda, Troast, Dawn M, Wiggin, Giselle, Zhang, Jing, Zhang, Ying, Clark, Matthew A

“…The discovery of ligands via affinity-mediated selection of DNA-encoded chemical libraries is driven by the quality and concentration of the protein target…”
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Sequenced Reactions with Samarium(II) Iodide. Sequential Intramolecular Reformatsky/Nucleophilic Acyl Substitution Reactions for the Synthesis of Medium-Sized Carbocycles by Molander, Gary A, Brown, Giles A, Storch de Gracia, Isabel

“…Samarium(II) iodide was used to access eight- and nine-membered carbocycles via a domino reaction comprised of a Reformatsky reaction followed by a…”
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