Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Peter Lockey"'
Autor:
Dennis Norman, Helen E. Colley, Munitta Muthana, Lynne Williams, Joanne Harrison, Sean F. Coole, Mark J. Thompson, Edward Jolyon Griffen, Matthew L. Brett, Sarah Danson, Vamshi Tulasi, Lucinda V. Jackson, Peter Lockey, Melanie Wong, Daniel P. Mason, Luke Jennings, Alexander G. Dossetter
Publikováno v:
Journal of Medicinal Chemistry. 58:9309-9333
A number of indole-3-glyoxylamides have previously been reported as tubulin polymerization inhibitors, although none has yet been successfully developed clinically. We report here a new series of related compounds, modified according to a strategy of
Autor:
Adam R. Johnson, Justin Lesch, Christine Everett, Harvey Wong, Susan Summerhill, Peter Lockey, Arunima Ganguli, Julie Hawkins, Benjamin Fauber, Jason DeVoss, Olivier Rene, Maxine Norman, Hank La, Yuzhong Deng, Celine Eidenschenk, Wenjun Ouyang, Alberto Gobbi
Publikováno v:
Journal of Medicinal Chemistry. 58:5308-5322
Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse ag
Autor:
Sarah G. Hymowitz, Alberto Gobbi, Gladys de Leon Boenig, Adam R. Johnson, Benjamin Fauber, Marya Liimatta, Celine Eidenschenk, Olivier Rene, Wenjun Ouyang, Peter Lockey, James R. Kiefer, Christine Everett, Heidi J.A. Wallweber, Brenda Burton, Harvey Wong, Maxine Norman
Publikováno v:
ACS Medicinal Chemistry Letters. 6:276-281
A minor structural change to tertiary sulfonamide RORc ligands led to distinct mechanisms of action. Co-crystal structures of two compounds revealed mechanistically consistent protein conformational changes. Optimized phenylsulfonamides were identifi
Autor:
Maxine Norman, Julie Hawkins, Olivier Rene, Benjamin Fauber, Adam R. Johnson, Peter Lockey, Marya Liimatta, Brenda Burton, Alberto Gobbi, Christine Everett, Harvey Wong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2182-2187
Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Herein, we describe the identification of compounds with improved RORc biochemical inverse agonist activity and cellular po
Autor:
Marcel J. de Groot, Karen Maubach, Neil Victor Harris, Kenneth Lyle Clark, Andrea Taylor, Peter Lockey, Christopher Higgs, Amanda J. Woodrooffe, R.A. Coleman, Richard Jon Davis, Jon Sutton, David E. Clark
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2212-2221
In this Letter, we present the results of a hit-finding and lead optimization programme against the EP4 receptor (EP4R). In a short time period, we were able to discover five structurally diverse series of hit compounds using a combination of virtual
Autor:
Harvey Wong, Celine Eidenschenk, Peter Lockey, Sarah G. Hymowitz, Christine Everett, Olivier Rene, Wenjun Ouyang, Maxine Norman, Marya Liimatta, Adam R. Johnson, Alberto Gobbi, Benjamin Fauber, Gladys de Leon Boenig, Brenda Burton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6604-6609
The structure-activity relationships of T0901317 analogs were explored as RORc inverse agonists using the principles of property- and structure-based drug design. An X-ray co-crystal structure of T0901317 and RORc was obtained and provided molecular
Autor:
Brenda Burton, Peter Lockey, Maxine Norman, Gary Jones, Adam R. Johnson, Olivier Rene, Stephen Bowerman, Harvey Wong, Gareth Harrold, Annerley Flynn, Adam Colebrook, Benjamin Fauber, Steve Huhn
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 57:57-60
The synthesis and characterization of [3H2]T0901317 and a structural isomer are described. The structural assignments of the closely related labeled compounds were primarily accomplished via 19F NMR analyses of the corresponding ethanolic compound di
Autor:
Sajad Mohammed, George Hynd, Nicholas C. Ray, Hazel Hunt, Shahadat Ahmed, Steve Daly, Peter Lockey, Gerry Buckley, Robert Roe, Jon Sutton, Robin D. Clark, Christine Blasey, Joe Belanoff, Elizabeth O'connor
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7376-7380
We report the optimization of a series of non-steroidal GR antagonists that led to the identification of compound 7. This compound is efficacious when dosed orally in an olanzapine-induced weight gain model in rats.
Autor:
Jonathan Gilley, Robert Adalbert, Jonathan Clark, Bohdan Waszkowycz, Melanie Wong, David E. Clark, Peter Lockey, Michael P. Coleman
Publikováno v:
Clark, D E, Waszkowycz, B, Wong, M, Lockey, P M, Adalbert, R, Gilley, J, Clark, J & Coleman, M P 2016, ' Application of virtual screening to the discovery of novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with potential for the treatment of cancer and axonopathies ', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 12, pp. 2920-2926 . https://doi.org/10.1016/j.bmcl.2016.04.039
NAMPT may represent a novel target for drug discovery in various therapeutic areas, including oncology and inflammation. Additionally, recent work has suggested that targeting NAMPT has potential in treating axon degeneration. In this work, publicly
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76067925156b34bd3fe4c153740dcd0e
https://www.repository.cam.ac.uk/handle/1810/276166
https://www.repository.cam.ac.uk/handle/1810/276166
Autor:
Gill Matthew Iain Andrew, Nigel Ramsden, Steve Price, Christopher Higgs, Richard Hale, Dennis Norman, Dan Leggate, Hazel Joan Dyke, Soraya S. Porres, Raffaella Mangano, Pascal Savy, Alison Jones, Francis Xavier Wilson, Peter Lockey, Neil Jennings, David E. Clark, Sue Cramp, Marie Andersson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2516-2519
The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H4 receptor inverse agonists is described. The initial hit, 3A (IC50 19 nM) was identified by means of a ligand-based virtual screening approach. Subs