Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Darren Le Grand"'
Autor:
Giles Pergl-Wilson, Anna King, Julia Hatto, Henry Danahay, David Andrew Sandham, Mariana Oana Popa, Emily Stanley, Parmjit Bahra, Urs Baettig, Rebecca Butler, Brian Cox, Lightfoot Megan, Christopher J. Page, Alice Young, Paul J. Groot-Kormelink, Trixie Wagner, Swarupa Kulkarni, Glyn Hughes, Edward Charles Hall, David J. Rowlands, Lee Edwards, Atwood K. Cheung, Matthew Spendiff, Tom Sharp, Kamlesh Bala, Stephen Paul Collingwood, Hazel Watson, Julia Koehler, Oliver Ross Steward, Anne-Lise Glotin, Penny Wright, Cara E. Brocklehurst, Ulrike Glaenzel, Ian Nicholls, Richard I. Robinson, Roger J. Taylor, Catherine Howsham, Brian Everatt, Darren Le Grand, Hedaythul Choudhury, Gareth Williams, Emma Budd, Martin Gosling, Pamela Tranter
Publikováno v:
Journal of Medicinal Chemistry. 64:7241-7260
Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel are established as the primary causative factor in the devastating lung disease cystic fibrosis (CF). More recently, cigarette smoke exposure has been shown to be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::795fc619db3aa5e70b7fe14aeddd53fe
https://doi.org/10.1021/acs.jmedchem.1c00343
https://doi.org/10.1021/acs.jmedchem.1c00343
Autor:
Mark Freeman, Victoria Head, Binesh Shrestha, Michael Faller, Elizabeth Hardaker, Mark R Dowling, Rene Hemmig, Lucy Elphick, Johan C. Hill, Darren Le Grand, David D. Pascoe, Florence Zink, Christopher Thomson, Andrew Lister, S. Rieffel, David Beattie, Oliver Ross Steward
Publikováno v:
Bioorganicmedicinal chemistry letters. 31
A series of inhibitors of Autotaxin (ATX) have been developed from a high throughput screening hit, 1a, which shows an alternative binding mode to known catalytic site inhibitors. Selectivity over the hERG channel and microsomal clearance were depend
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02e384195e054e5c4b466872e8c04973
https://pubmed.ncbi.nlm.nih.gov/33160025
https://pubmed.ncbi.nlm.nih.gov/33160025
Publikováno v:
ACS Chem Biol
Tyrosyl DNA phosphodiesterase 2 (TDP2) facilitates the repair of topoisomerase II (TOP2)-linked DNA double-strand breaks and, as a consequence, is required for cellular resistance to TOP2 "poisons". Recently, a deazaflavin series of compounds were id
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d47043a8faf5d2d428db9c8a62a469a
https://pubmed.ncbi.nlm.nih.gov/31091068
https://pubmed.ncbi.nlm.nih.gov/31091068
Autor:
Angeliki Ditsiou, Georgios Giamas, Chrisostomos Prodromou, Jose Gascon, Teresa Gagliano, Sophie Mumford, Darren Le Grand
Publikováno v:
Endocrine Abstracts.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8e5282af821f4519ae8c90be7f8195f3
https://doi.org/10.1530/endoabs.56.p651
https://doi.org/10.1530/endoabs.56.p651
Autor:
Darren Le Grand, Jessica Hudson, Hitesh Patel, Simon E. Ward, Andrea Gunnell, Lewis E. Pennicott, Katie Duffell, Jessica A. Downs, Jessica R Booth, Kay Osborn
Publikováno v:
Cancer Research. 78:2907-2907
Gene expression frequently requires the dynamic remodelling of the chromatin architecture to orchestrate the assembly of transcriptional protein complexes at the promoter sites of DNA. Chromatin remodelling complexes are multicomponent proteins that
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::65316d5effbdf4c1fef8ab9a4393b480
https://doi.org/10.1158/1538-7445.am2018-2907
https://doi.org/10.1158/1538-7445.am2018-2907
Autor:
Mohan B. Rajasekaran, Tristan Reuillon, Darren Le Grand, Antony W. Oliver, Ben Wahab, Simon E. Ward, Sarah R. Walker, Helfrid Hochegger
Publikováno v:
Cancer Research. 77:4210-4210
MASTL (microtubule-associated serine/threonine kinase-like), commonly known as Greatwall (GWL), is a member of the AGC kinase family and has recently emerged as a novel cancer therapy target. GWL regulates mitotic division via phosphorylation of its
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e5cd2312494751755f115551406e3c13
https://doi.org/10.1158/1538-7445.am2017-4210
https://doi.org/10.1158/1538-7445.am2017-4210
Autor:
Darryl Brynley Jones, Karen Dunnet, John Ambler, Lyndon Nigel Brown, Diana Janus, Garrick Smith, Dave Bentley, Mark Mercer, Keith Menear, Dave Farr, K D Butler, Paul Butler, Morris Tweed, Emma Baker, Mark Talbot, Darren Le Grand, Judy Hayler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:737-742
The application of selection criteria, based on potency and physicochemical parameters, to a candidate library of thrombin inhibitors is described. The utility of the approach is exemplified by the discovery of a potent, selective and bioavailable th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b71e74af7c3708ef01cda36045d1146
https://doi.org/10.1016/s0960-894x(99)00061-x
https://doi.org/10.1016/s0960-894x(99)00061-x
Autor:
Nicola Elaine Press, Clive Mccarthy, Ian N. Bruce, Lewis Whitehead, Lilya Sviridenko, Mrinalini Sachin Oza, Gaynor Elizabeth Pilgrim, Darren Le Grand, Charles Owen, Louise Kirman, Graham Charles Bloomfield, Thomas H. Keller, Peter Finan, Judy Hayler, Mohammed Akhlaq, Denise Head, Emma Budd, Julia Hatto, Bernard Cuenoud, Peter Gedeck, Desmond O'Connor, Brian Cox, Catherine Leblanc
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(17)
Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e876bd0609cb94ac31c0d54a9c921ed8
https://pubmed.ncbi.nlm.nih.gov/22863202
https://pubmed.ncbi.nlm.nih.gov/22863202
Autor:
Darren Le Grand, et al. et al.
Publikováno v:
ChemInform. 30
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::90de30afc9ce88c7c7554cfee4ad3b57
https://doi.org/10.1002/chin.199932202
https://doi.org/10.1002/chin.199932202
Autor:
Lyndon Nigel Brown, Keith Menear, Dave Farr, Darren Le Grand, Morris Tweed, John Ambler, Karen Dunnet, Mark Mercer, Diana Janus, Bernard Wathey, David Bentley, Mark Talbot
Publikováno v:
Bioorganicmedicinal chemistry letters. 9(8)
Thrombin inhibitors have been designed with the replacement of the strongly basic guanidine P1 pharmocophore with a group that exploits the lipophilicity of the S1 pocket. The approach has lead to the discovery of potent thrombin inhibitors demonstra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e2adac2f91335be131c61084027db0e
https://pubmed.ncbi.nlm.nih.gov/10328293
https://pubmed.ncbi.nlm.nih.gov/10328293