Zobrazeno 1 - 10
of 110
pro vyhledávání: '"Miles Congreve"'
Autor:
Charlotte Bakker, Tim Tasker, Jan Liptrot, Ellen P. Hart, Erica S. Klaassen, Robert Jan Doll, Giles A. Brown, Alastair Brown, Miles Congreve, Malcolm Weir, Fiona H. Marshall, David M. Cross, Geert Jan Groeneveld, Pradeep J. Nathan
Publikováno v:
Alzheimer’s Research & Therapy, Vol 13, Iss 1, Pp 1-19 (2021)
Abstract Background The cholinergic system and M1 receptor remain an important target for symptomatic treatment of cognitive dysfunction. The selective M1 receptor partial agonist HTL0018318 is under development for the symptomatic treatment of Demen
Externí odkaz:
https://doaj.org/article/8f25b2ca13ee46c9988b118de2ad5f58
Autor:
Pradeep J. Nathan, S. Babli Millais, Alex Godwood, Odile Dewit, David M. Cross, Janet Liptrot, Bharat Ruparelia, Stephen Paul Jones, Geor Bakker, Paul T. Maruff, Gregory A. Light, Alastair J.H. Brown, Malcolm Peter Weir, Miles Congreve, Tim Tasker
Publikováno v:
Alzheimer’s & Dementia: Translational Research & Clinical Interventions, Vol 8, Iss 1, Pp n/a-n/a (2022)
Abstract Introduction This study examined the safety and pharmacodynamic effects of selective muscarinic M1 receptor orthosteric agonist HTL0018318 in 60 patients with mild‐to‐moderate Alzheimer's disease (AD) on background donepezil 10 mg/day. M
Externí odkaz:
https://doaj.org/article/d2ea8035b82442a48e018eec2348acbe
Autor:
Yanjun Wang, James Brown, Richard Woessner, Alwin G Schuller, Alexandra Borodovsky, Dinesh Chandra, Deanna A Mele, Stephen Fawell, Joseph Shaw, Christine M Barbon, Minwei Ye, Laura Prickett, Nanhua Deng, Kris Sachsenmeier, James D Clarke, Bolan Linghu, Giles A Brown, Miles Congreve, Robert KY Cheng, Andrew S Dore, Edward Hurrell, Wenlin Shao, Corinne Reimer, Lisa Drew
Publikováno v:
Journal for ImmunoTherapy of Cancer, Vol 8, Iss 2 (2020)
Methods We report here the development of a small molecule A2AR inhibitor including characterization of binding and inhibition of A2AR function with varying amounts of a stable version of adenosine. Functional activity was tested in both mouse and hu
Externí odkaz:
https://doaj.org/article/84f658f3a812430ca348354c04f4101a
Autor:
Andrew D. Cansfield, Mark A. Ator, Joydeep Banerjee, Michael Bestwick, Andrea Bortolato, Giles A. Brown, Jason Brown, Kristina Butkovic, Julie E. Cansfield, John A. Christopher, Miles Congreve, Gabriella Cseke, Francesca Deflorian, Benjamin Dugan, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Goran Landek, Jonathan Mason, Alistair O’Brien, Gregory R. Ott, Renata Rupcic, Gordon Saxty, Stacey M. Southall, Rahela Zadravec, Stephen P. Watson
Publikováno v:
ACS Chemical Neuroscience. 13:751-765
A series of macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonists identified using structure-based design principles, exemplified by HTL0028016 (1) and HTL0028125 (2), is described. Structural characterization by X-ray crystallograp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c446db762c3a729f140cd365a9977f1b
https://doi.org/10.1021/acschemneuro.1c00696
https://doi.org/10.1021/acschemneuro.1c00696
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery. :1-59
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::32c7f32e87b8e3275d504dce6c7b6f9a
https://doi.org/10.1002/0471266949.bmc269
https://doi.org/10.1002/0471266949.bmc269
Autor:
Andrew B. Tobin, Gerard R. Dawson, Patrick M. Sexton, Nathan Robertson, Sophie J. Bradley, Francesca Perini, Arthur Christopoulos, James C. Errey, Barry John Teobald, John Francis William Deakin, Lisa M. Broad, Jan Liptrot, Christopher J. Langmead, K.A. Bennett, Mary Vinson, Pradeep J. Nathan, Colin Molloy, Robert M. Cooke, Edward Hurrell, Michael Browning, Krzysztof Okrasa, Jason M Brown, Giulio Mattedi, Alastair J. H. Brown, David M. Cross, Greg J. Osborne, Julie E. Cansfield, Ali Jazayeri, Christoffer Bundgaard, Stephen R. Morairty, J.C. Patel, Fiona H. Marshall, Brian D. Hudson, Prakash Rucktooa, Robert T. Smith, Keith G. Phillips, Louis Dwomoh, Chris de Graaf, Malcolm Peter Weir, Julie Warneck, Giles A. Brown, Mark Pickworth, Benjamin G. Tehan, Tim Tasker, Anushka V. Goonawardena, Miles Congreve, João M. Dias, Shahram Shahabi
Current therapies for Alzheimer's disease seek to correct for defective cholinergic transmission by preventing the breakdown of acetylcholine through inhibition of acetylcholinesterase, these however have limited clinical efficacy. An alternative app
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b008b7a3c01abe25b8e63fdab465cc4
https://ora.ox.ac.uk/objects/uuid:fc10e298-8675-4411-9af5-3cfd801f0d78
https://ora.ox.ac.uk/objects/uuid:fc10e298-8675-4411-9af5-3cfd801f0d78
Autor:
María Majellaro, Robert M. Cooke, Andrei Zhukov, Andrew S. Doré, Francesca Deflorian, Henrik Keränen, Hugo Gutiérrez-de-Terán, Grégory Verdon, Miles Congreve, Johan Åqvist, Eddy Sotelo, Jhonny Azuaje, Xerardo García-Mera, Chris de Graaf, Willem Jespers, Jonathan S. Mason
Publikováno v:
Angewandte Chemie (International Ed. in English)
Minerva: Repositorio Institucional de la Universidad de Santiago de Compostela
Universidad de Santiago de Compostela (USC)
Minerva. Repositorio Institucional de la Universidad de Santiago de Compostela
instname
Minerva: Repositorio Institucional de la Universidad de Santiago de Compostela
Universidad de Santiago de Compostela (USC)
Minerva. Repositorio Institucional de la Universidad de Santiago de Compostela
instname
We present a robust protocol based on iterations of free energy perturbation (FEP) calculations, chemical synthesis, biophysical mapping and X‐ray crystallography to reveal the binding mode of an antagonist series to the A2A adenosine receptor (AR)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fb82a0e9f21ff3cb50f65224bd63c71
https://doi.org/10.1002/anie.202003788
https://doi.org/10.1002/anie.202003788
Autor:
Gary Tresadern, Herman van Vlijmen, Jonathan S. Mason, Eelke B. Lenselink, Francesca Deflorian, Chris de Graaf, Laura Pérez-Benito, Miles Congreve
Publikováno v:
Journal of Chemical Information and Modeling. 60:5563-5579
The computational prediction of relative binding free energies is a crucial goal for drug discovery, and G protein-coupled receptors (GPCRs) are arguably the most important drug target class. However, they present increased complexity to model compar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcfaf71e98d0403c4ea3cb62fb061f19
https://doi.org/10.1021/acs.jcim.0c00449
https://doi.org/10.1021/acs.jcim.0c00449
Autor:
Jack R. Mellor, Benjamin G. Tehan, Miles Congreve, Alastair J. H. Brown, Pradeep J. Nathan, Matt Udakis, Giles Albert Brown, Jon Palacios-Filardo
Publikováno v:
Palacios-Filardo, J, Udakis, M, Mellor, J R & al., E 2021, ' Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits ', Nature Communications, vol. 12, no. 1, 5475 . https://doi.org/10.1038/s41467-021-25280-5
Nature Communications
Nature Communications, Vol 12, Iss 1, Pp 1-16 (2021)
Nature Communications
Nature Communications, Vol 12, Iss 1, Pp 1-16 (2021)
Funder: Biotechnology and Biological Sciences Research Council
Acetylcholine release in the hippocampus plays a central role in the formation of new memory representations. An influential but largely untested theory proposes that memory formatio
Acetylcholine release in the hippocampus plays a central role in the formation of new memory representations. An influential but largely untested theory proposes that memory formatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5bafd7502f86d226d45b37546b720de6
https://www.repository.cam.ac.uk/handle/1810/331856
https://www.repository.cam.ac.uk/handle/1810/331856
Autor:
Pradeep J, Nathan, S Babli, Millais, Alex, Godwood, Odile, Dewit, David M, Cross, Janet, Liptrot, Bharat, Ruparelia, Stephen Paul, Jones, Geor, Bakker, Paul T, Maruff, Gregory A, Light, Alastair J H, Brown, Malcolm Peter, Weir, Miles, Congreve, Tim, Tasker
Publikováno v:
Alzheimer'sdementia (New York, N. Y.). 8(1)
This study examined the safety and pharmacodynamic effects of selective muscarinic MA randomized, double-blind, placebo-controlled 4-week safety study of HTL0018318 with up-titration and maintenance phases, observing exploratory effects on electrophy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ad0c05b300f87c734f6afd7887305f6d
https://pubmed.ncbi.nlm.nih.gov/35229025
https://pubmed.ncbi.nlm.nih.gov/35229025