Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Clare I. Hobbs"'
Autor:
Jonathan P. Hutchinson, Paul Rowland, Mark R. D. Taylor, Erica M. Christodoulou, Carl Haslam, Clare I. Hobbs, Duncan S. Holmes, Paul Homes, John Liddle, Damian J. Mole, Iain Uings, Ann L. Walker, Scott P. Webster, Christopher G. Mowat, Chun-wa Chung
Publikováno v:
Nature Communications, Vol 8, Iss 1, Pp 1-12 (2017)
Kynurenine-3-monooxygenase (KMO) is an emerging clinical target for treatment of neurodegenerative diseases and acute pancreatitis. Here, the authors report potent inhibitors that bind KMO in an unexpected conformation, offering structural and mechan
Externí odkaz:
https://doaj.org/article/6a2d1e05cbf54050aa6e26f4834e4b9a
Autor:
Duncan S. Holmes, Paul Homes, Chun-wa Chung, Ann Louise Walker, Jonathan P. Hutchinson, Erica Christodoulou, John Liddle, Christopher G. Mowat, Scott P. Webster, Iain Uings, Carl Haslam, Clare I. Hobbs, Damian J. Mole, Paul Rowland, Mark R D Taylor
Publikováno v:
Nature Communications, Vol 8, Iss 1, Pp 1-12 (2017)
Hutchinson, J P, Rowland, P, Taylor, M R D, Christodoulou, E M, Haslam, C, Hobbs, C M, Holmes, D, Homes, P, Liddle, J, Mole, D J, Uings, I J, Walker, A L, Webster, S P, Mowat, C & Chung, C 2017, ' Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase ', Nature Communications, vol. 8, 15827 . https://doi.org/10.1038/ncomms15827
Nature Communications
'Nature Communications ', vol: 8, pages: 15827-1-15827-12 (2017)
Hutchinson, J P, Rowland, P, Taylor, M R D, Christodoulou, E M, Haslam, C, Hobbs, C M, Holmes, D, Homes, P, Liddle, J, Mole, D J, Uings, I J, Walker, A L, Webster, S P, Mowat, C & Chung, C 2017, ' Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase ', Nature Communications, vol. 8, 15827 . https://doi.org/10.1038/ncomms15827
Nature Communications
'Nature Communications ', vol: 8, pages: 15827-1-15827-12 (2017)
Kynurenine-3-monooxygenase (KMO) is a key FAD-dependent enzyme of tryptophan metabolism. In animal models, KMO inhibition has shown benefit in neurodegenerative diseases such as Huntington's and Alzheimer's. Most recently it has been identified as a
Autor:
Laurie J. Gordon, David J. Fallon, Heather A. Barnett, Chun-wa Chung, Darren Jason Mitchell, Emma J. Jones, Robert J. Watson, Rab K. Prinjha, Armelle Le Gall, Isabelle Becher, Paola Grandi, Emmanuel Hubert Demont, Edward Hooper-Greenhill, Peter D. Craggs, Mark J. Bird, Allan J. B. Watson, Hawa Diallo, Robert P. Law, Robert J. Sheppard, Anne-Marie Michon, Dave Lugo, Paul Bamborough, Clare I. Hobbs
Publikováno v:
ACS Medicinal Chemistry Letters. 7:552-557
The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target
Autor:
Emmanuel Hubert Demont, Robert J. Sheppard, Paola Grandi, Clare I. Hobbs, Chun-wa Chung, Peter D. Craggs, Jameed Hussain, Darren Jason Mitchell, Laurie J. Gordon, Paul Bamborough, Armelle Le Gall, David J. Fallon, Andrew D. Roberts, Rab K. Prinjha, Emma J. Jones, Robert J. Watson, Anne-Marie Michon
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1190-1195
The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the
Autor:
Svetlana L. Belyanskaya, Chun-wa Chung, Eric Humphries, Christopher S. Kollmann, Nicolas Ancellin, Christopher C. Arico-Muendel, Hongfeng Deng, Ryan P. Bingham, Van Loc Nguyen, Jeffrey A. Messer, Yun Ding, Emily Blazensky, Arthur Beljean, Anne-Benedicte Boullay, Sarah E. Smith, Jingye Zhou, Edwige Nicodeme, Jing Chai, Flora S. Sundersingh, Clare I. Hobbs, Alain Claude-Marie Daugan, Myriam Ajakane, Donald O. Somers, Nerina Dodic, Kenny Herry, Paul S. Carter, Eric Boursier
To identify BCATm inhibitors suitable for in vivo study, Encoded Library Technology (ELT) was used to affinity screen a 117 million member benzimidazole based DNA encoded library, which identified an inhibitor series with both biochemical and cellula
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19d2b0e96f6386d1d5d0d6f742324e42
https://europepmc.org/articles/PMC4834658/
https://europepmc.org/articles/PMC4834658/
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
Autor:
Angela M. Deakin, Erik Schaefer, Paolo Luraghi, Min Li, Clare I. Hobbs, Vipul K. Patel, Augustin Amour, Mark Surby, Xiao Dong Qian, Jane Denyer, C. J. Clark, Paul S. Carter
Publikováno v:
Analytical Biochemistry. 384:56-67
Spleen tyrosine kinase (Syk) is involved in the activation of cells implicated in allergic or autoimmune diseases and certain cancers. Therefore, Syk inhibitors may prove to be effective in treating diseases where Syk activity or expression is increa
Autor:
Laura J Pothier Kaushansky, Jennifer L. DeLorey, Hongfeng Deng, Christopher P. Davie, Jingye Zhou, Sarah E. Smith, Katie L Sargent Bedard, Christopher S. Kollmann, Barry A. Morgan, Nicolas Ancellin, Kenny Herry, Matthew A. Clark, Eric Boursier, Paul S. Carter, Clare I. Hobbs, Quan Zhou, Alexander L. Satz, Don O. Somers, Svetlana L. Belyanskaya, Jeffrey A. Messer, Yun Ding, Flora S. Sundersingh, Arthur Beljean, Chun-wa Chung, Ryan P. Bingham, LaShadric C. Grady, Christopher C. Arico-Muendel, G Joseph Franklin, Paolo A. Centrella, Jennifer Summerfield
As a potential target for obesity, human BCATm was screened against more than 14 billion DNA encoded compounds of distinct scaffolds followed by off-DNA synthesis and activity confirmation. As a consequence, several series of BCATm inhibitors were di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1887eff01483569c140544dbed75f5c
https://europepmc.org/articles/PMC4538436/
https://europepmc.org/articles/PMC4538436/
Autor:
Ian Churcher, Sarah E. Smith, Ryan P. Bingham, Clare I. Hobbs, Donald O. Somers, Eric Boursier, Chun Wa Chung, Charlène Fournier, Yoshiaki Washio, Peter Francis, Claus Spitzfaden, Iain H. Reid, Stephen D. Pickett, Sophie M. Bertrand, Graham L. Simpson, Andrew N. Hobbs, Klára Valkó, Laura A. Gummer, Robert J. Young, Nicolas Ancellin, Craig Jamieson, Colin J. Suckling, Anne Bénédicte Boullay, Lisa A. Sloan, Kenny Herry, Paul S. Carter, Nerina Dodic, Paul Homes, Edwige Nicodeme, Jennifer A. Borthwick, Benjamin Beaufils, Marie Helene Fouchet
Publikováno v:
Journal of medicinal chemistry. 58(18)
The hybridization of hits, identified by complementary fragment and high throughput screens, enabled the discovery of the first series of potent inhibitors of mitochondrial branched-chain aminotransferase (BCATm) based on a 2-benzylamino-pyrazolo[1,5
Autor:
Sophie M. Bertrand, Nicolas Ancellin, Benjamin Beaufils, Ryan P. Bingham, Jennifer A. Borthwick, Anne-Bénédicte Boullay, Eric Boursier, Paul S. Carter, Chun-wa Chung, Ian Churcher, Nerina Dodic, Marie-Hélène Fouchet, Charlène Fournier, PeterL. Francis, Laura A. Gummer, Kenny Herry, Andrew Hobbs, Clare I. Hobbs, Paul Homes, Craig Jamieson
Publikováno v:
Journal of Medicinal Chemistry; Sep2015, Vol. 58 Issue 18, p7140-7163, 24p