Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Cesar Ramirez-Molina"'
Autor:
Philip G. Humphreys, Niall A. Anderson, Paul Bamborough, Andrew Baxter, Chun-wa Chung, Rosa Cookson, Peter D. Craggs, Toryn Dalton, Julie C. L. Fournier, Laurie J. Gordon, Heather F. Gray, Matthew W. Gray, Richard Gregory, David J. Hirst, Craig Jamieson, Katherine L. Jones, Hripsimee Kessedjian, David Lugo, Grant McGonagle, Vipulkumar K. Patel, Christopher Patten, Darren L. Poole, Rab K. Prinjha, Cesar Ramirez-Molina, Inmaculada Rioja, Gail Seal, Kayleigh A. J. Stafford, Rishi R. Shah, Daniel Tape, Natalie H. Theodoulou, Laura Tomlinson, Sabri Ukuser, Ian D. Wall, Natalie Wellaway, Gemma White
Publikováno v:
Journal of Medicinal Chemistry. 65:15174-15207
The bromodomain and extra terminal (BET) family of proteins are an integral part of human epigenome regulation, the dysregulation of which is implicated in multiple oncology and inflammatory diseases. Disrupting the BET family bromodomain acetyl-lysi
Autor:
Michael David Barker, Emma J. Jones, Robert J. Watson, Huw D. Lewis, Cesar Ramirez-Molina, David Matthew Wilson, Marion C. Dickson, Robert P. Davis, Francis Louis Atkinson, Margarete Neu, Donald O. Somers, John Liddle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3458-3462
The discovery and lead optimisation of a novel series of SYK inhibitors is described. These were optimised for SYK potency and selectivity against Aurora B. Compounds were profiled in a human skin penetration study to identify a suitable candidate mo
FSO systems present many advantages like high data rate, license-free bandwidth and tap-proof communication allowing the download of vast amounts of data from LEO satellites. However, the atmospheric channel is quite challenging, because of spurious
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e52143e8470080499daafcde857171e
https://elib.dlr.de/136480/
https://elib.dlr.de/136480/
Autor:
Aoife Ward, Dean Tyler, Sarah-Jane Dawson, Edwin D. Hawkins, Paola Grandi, Dave Lugo, Johanna Vappiani, Richard Gregory, Anna Rutkowska, Tatiana Cañeque, Susan Jackson, Cesar Ramirez Molina, Antje Hienzsch, Anne J. Wagner, Rab K. Prinjha, Mark A. Dawson, Thilo Werner, Neil Stuart Garton, Charles C. Bell, Christopher Roland Wellaway, Omer Gilan, Colin M. House, Margarida Figueiredo, Yih-Chih Chan, Gerard Drewes, Raphaël Rodriguez, Laura MacPherson, Sabine Stolzenburg, Enid Y.N. Lam
Publikováno v:
Science
Are better drugs just a click away? Drugs that show promise in preclinical models often fail in the clinic, in part because of limited information on drug localization within cells and across tissues. In a proof-of-concept study, Tyler et al. applied
Autor:
Alex Preston, Scott McCleary, Emma J. Jones, Huw D. Lewis, Michael David Barker, Robert J. Watson, Tracy Jane Shipley, Cesar Ramirez-Molina, Dave Lugo, Clement Douault, Robert P. Davis, David Matthew Wilson, Margarete Neu, Neil Stuart Garton, Edward Hooper-Greenhill, John Liddle, Don O. Somers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4606-4612
The optimisation of the azanaphthyridine series of Spleen Tyrosine Kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over hERG activity. A go
Autor:
Marion C. Dickson, Sidsel Falkencrone, Cesar Ramirez Molina, Edward Hooper-Greenhill, Mike Barker, Per Stahl Skov
Publikováno v:
British journal of pharmacology. 176(8)
BACKGROUND AND PURPOSE: Chronic spontaneous urticaria presents as a heterogeneous syndrome characterised by wheals, angioedema, or both for greater than 6 weeks. Spleen tyrosine kinase mediates allergen‐induced mast cell degranulation via the IgE s
Autor:
Kevin Lee, Pedro J. Gomez-Pinilla, Cesar Ramirez-Molina, Fleur Suzanne van de Bovenkamp, Michael J. Skynner, Wouter J de Jonge, Sjoerd H. van Bree, Martina Di Giovangiulio, Cathy Cailotto, Dave Lugo, Andrea Nemethova, G. E. E. Boeckxstaens, Giovanna Farro, Gianluca Matteoli
Publikováno v:
Gut, 62(11), 1581-1590. BMJ Publishing Group
OBJECTIVE: Intestinal inflammation resulting from manipulation-induced mast cell activation is a crucial mechanism in the pathophysiology of postoperative ileus (POI). Recently it has been shown that spleen tyrosine kinase (Syk) is involved in mast c
Autor:
Catherine Swales, Angela Bridges, Chun-wa Chung, Kevin Lee, Marcus Bantscheff, Dirk Eberhard, Julia Smith, John Liddle, Paul Rowland, C. Bountra, Robert J. Sheppard, Palwinder K. Mander, Emma J. Jones, Dinshaw J. Patel, Sue Hutchinson, Gerard Drewes, J. Mosley, Cesar Ramirez-Molina, Pamela Thomas, Laurens Kruidenier, Roy Katso, K.H. Che, Zhongjun Cheng, Christopher J. Schofield, Gerard Joberty, Hawa Diallo, Melanie Leveridge, Anthony Tumber, Robert Tanner, Udo Oppermann, David Matthew Wilson
Publikováno v:
Nature, vol 488, iss 7411
The jumonji (JMJ) family of histone demethylases are Fe2+- and α-ketoglutarate-dependent oxygenases that are essential components of regulatory transcriptional chromatin complexes. These enzymes demethylate lysine residues in histones in a methylati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e039405fd27845021f2d7f05d369eb4d
https://doi.org/10.1038/nature11262
https://doi.org/10.1038/nature11262
Autor:
Heather Hobbs, Rick P. C. Cousins, Caroline Whitworth, Ruth R. Osborn, Cesar Ramirez-Molina, Giorgia Vicentini, Chris Ioannou, Chun-wa Chung, Jeremy John Payne, Michelle L. Heathcote, Michael David Barker, Sebastien Andre Campos, Paul Faulder, Mary A. Morse, William L. Rumsey, John Liddle, Daniel Terence Tape, John Martin Pritchard, Rick Williamson, Duncan S. Holmes, Paul Bamborough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5222-5226
The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good ef
Autor:
Philip Alan Skone, Donald O. Somers, Marion C. Dickson, Nick Smithers, Ann Louise Walker, Thomas George Christopher Hayhow, Stuart G. Leach, Karen Leavens, Clement Douault, Emma J. Jones, Dorothy Elwes, Robert J. Watson, Margarete Neu, Robert P. Davis, Matthew Gray, Neil Stuart Garton, Clare I. Hobbs, Alex Preston, Michael David Barker, Vipulkumar Kantibhai Patel, Cesar Ramirez-Molina, Paul S. Carter, Scott McCleary, Gordon G. Weingarten, Huw D. Lewis, Francis Louis Atkinson, John Liddle, Tracy Jane Shipley, Neil R. Curtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6188-6194
The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over l