Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Emma J. Jones"'
Autor:
Max Pearson, Carl Haslam, Andrew Fosberry, Emma J. Jones, Mark Reglinski, Lucy Reeves, Robert J. Edwards, Richard Ashley Lawrenson, Jonathan C. Brown, Danuta Mossakowska, James Edward Pease, Shiranee Sriskandan
Publikováno v:
Scientific Reports, Vol 13, Iss 1, Pp 1-9 (2023)
Abstract The Streptococcus pyogenes cell envelope protease (SpyCEP) is vital to streptococcal pathogenesis and disease progression. Despite its strong association with invasive disease, little is known about enzymatic function beyond the ELR+ CXC che
Externí odkaz:
https://doaj.org/article/217b26e4b24c411eae15df0e65268160
Autor:
Charles S. Lay, Daniel A. Thomas, John P. Evans, Emma J. Jones, Kelly M. Gatfield, Peter D. Craggs
Publikováno v:
STAR Protocols, Vol 3, Iss 1, Pp 101078- (2022)
Summary: The Kinetic Intra-Cellular Assay (KICA) is a recombinant cell-based technique that utilizes NanoBRET technology. KICA enables the measurement of intracellular binding kinetics. This protocol describes steps for cellular transfection and expr
Externí odkaz:
https://doaj.org/article/bef9a962d1c24509b55841d676162543
Autor:
Peter D. Craggs, Darren Jason Mitchell, Rab K. Prinjha, Alex Preston, James Michael Woolven, Laurie J. Gordon, Simon Taylor, Paul Bamborough, Chun-wa Chung, Paola Grandi, James Gray, Francesco Rianjongdee, Matthew J Lindon, Anne-Marie Michon, Emma J. Jones, Inmaculada Rioja, Robert J. Watson, Ian D. Wall, Stephen John Atkinson, Emmanuel Hubert Demont, Jonathan Thomas Seal
Publikováno v:
Journal of Medicinal Chemistry. 63:9070-9092
Pan-bromodomain and extra terminal domain (BET) inhibitors interact equipotently with the eight bromodomains of the BET family of proteins and have shown profound efficacy in a number of in vitro phenotypic assays and in vivo pre-clinical models in i
Non-conventional serine protease activity of the CXC chemokine-cleaving streptococcal enzyme, SpyCEP
Autor:
James E. Pease, Carl Haslam, Robert Edwards, Andrew P. Fosberry, Danuta Mossakowska, Emma J. Jones, Richard A. Lawrenson, Mark Reglinski, Max Pearson, Shiranee Sriskandan
The Streptococcus pyogenes cell envelope protease (SpyCEP) is a vital virulence factor in streptococcal pathogenesis. Despite its key role in disease progression and strong association with invasive disease, little is known about the enzymatic functi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::00bd6beb812107e2f750c7a93a457807
https://doi.org/10.1101/2021.11.14.468564
https://doi.org/10.1101/2021.11.14.468564
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
Autor:
Emma J. Jones, Charles S. Lay, Charlotte E. Carver, John P. Evans, Kristopher McCombe, Alexander N Phillipou, Daniel Thomas, Peter D. Craggs, Cassie Messenger, Mahnoor Mahmood, Kelly M Gatfield, Kristin M. Riching, Laurie J. Gordon, Matthew Campbell
Publikováno v:
Cell chemical biology. 29(2)
Contemporary drug discovery typically quantifies the effect of a molecule on a biological target using the equilibrium-derived measurements of IC50, EC50, or KD. Kinetic descriptors of drug binding are frequently linked with the effectiveness of a mo
Autor:
Alex, Preston, Stephen, Atkinson, Paul, Bamborough, Chun-Wa, Chung, Peter D, Craggs, Laurie, Gordon, Paola, Grandi, James R J, Gray, Emma J, Jones, Matthew, Lindon, Anne-Marie, Michon, Darren J, Mitchell, Rab K, Prinjha, Francesco, Rianjongdee, Inmaculada, Rioja, Jonathan, Seal, Simon, Taylor, Ian, Wall, Robert J, Watson, James, Woolven, Emmanuel H, Demont
Publikováno v:
Journal of medicinal chemistry. 63(17)
Pan-bromodomain and extra terminal domain (BET) inhibitors interact equipotently with the eight bromodomains of the BET family of proteins and have shown profound efficacy in a number of
Autor:
Jonathan D Lea, Robert J. Young, Duncan S. Holmes, Christopher P. Tinworth, Jonathan P. Hutchinson, Semra Kitchen, Justyna Wojno-Picon, Leng Nickels, Michelle Pemberton, Hester Sheehan, Justyna Korczynska, Margarete Neu, Jessica L. Schneck, Efstratios Stratikos, Despoina Koumantou, Iain Uings, Ted Cecconie, Alex Phillipou, Emma J. Jones, John Liddle, Paul Rowland
Publikováno v:
Journal of medicinal chemistry. 63(6)
ER aminopeptidase 1 (ERAP1) is an intracellular enzyme that generates antigenic peptides and is an emerging target for cancer immunotherapy and the control of autoimmunity. ERAP1 inhibitors described previously target the active site and are limited
Autor:
Cassie Messenger, Laurie J. Gordon, Simon C. C. Lucas, Aaron T. Cheng, Kelly M Gatfield, John P. Evans, Emma J. Jones, Mahnoor Mahmood, Charles S. Lay, Charlotte E. Carver, Douglas Sammon, Antonia J. Lewis, Alexander N Phillipou, Syandan Chakraborty, Luke A Greenhough, Peter D. Craggs, David J Brierley
Publikováno v:
SLAS discovery : advancing life sciences RD. 25(2)
Malfunctions in the basic epigenetic mechanisms such as histone modifications, DNA methylation, and chromatin remodeling are implicated in a number of cancers and immunological and neurodegenerative conditions. Within GlaxoSmithKline (GSK) we have ut
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