Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Rowena Callis"'
Autor:
Donald Ogilvie, Robert W. Wilkinson, Bernard Barlaam, Paul Smith, Konstantina Grosios, Elizabeth Mills, Rowena Callis, Sara Davenport, Gayle Marshall, Sarah Beck, Judith Anderton, Cath Trigwell, John Vincent, Georgina Speake, Teresa Klinowska, D. Mark Hickinson
Supplementary Data from AZD8931, an Equipotent, Reversible Inhibitor of Signaling by Epidermal Growth Factor Receptor, ERBB2 (HER2), and ERBB3: A Unique Agent for Simultaneous ERBB Receptor Blockade in Cancer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a7713f65d79a8772a0aabd9ebd0f375
https://doi.org/10.1158/1078-0432.22442994
https://doi.org/10.1158/1078-0432.22442994
Autor:
Donald Ogilvie, Robert W. Wilkinson, Bernard Barlaam, Paul Smith, Konstantina Grosios, Elizabeth Mills, Rowena Callis, Sara Davenport, Gayle Marshall, Sarah Beck, Judith Anderton, Cath Trigwell, John Vincent, Georgina Speake, Teresa Klinowska, D. Mark Hickinson
Purpose: To test the hypothesis that simultaneous, equipotent inhibition of epidermal growth factor receptor (EGFR; erbB1), erbB2 (human epidermal growth factor receptor 2), and erbB3 receptor signaling, using the novel small-molecule inhibitor AZD89
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc3df99d9418da872c459a0c2702594c
https://doi.org/10.1158/1078-0432.c.6519609.v1
https://doi.org/10.1158/1078-0432.c.6519609.v1
Autor:
Dmitri I. Svergun, Huawei Chen, Romel Bobby, Natalie Stratton, Danette L. Daniels, Scott Boiko, Rowena Callis, Yi Yao, Graeme R. Robb, Alfred A. Rabow, Mark S. B. McAlister, Graeme Walker, Joe Patel, Matthew B. Robers, Derek Ogg, Sakina Saif, Liz Flavell, Philip Petteruti, Austin Dulak, Ian L. Dale, Jacqui Méndez, Thomas A. Jowitt, Michael J. Waring, David Matthew Wilson, David Whittaker, Wenxian Wang, Edwin Clark, Alexey Kikhney, Geoff Holdgate, Rob H. Bradbury
Publikováno v:
Nature Chemical Biology. 12:1097-1104
Proteins of the bromodomain and extraterminal (BET) family, in particular bromodomain-containing protein 4 (BRD4), are of great interest as biological targets. BET proteins contain two separate bromodomains, and existing inhibitors bind to them monov
Autor:
Joe Patel, Mark A. Graham, Maureen Hattersley, Stephen Stokes, David Whittaker, Carr Gregory Richard, David Whalley, Edwin Clark, Craig A. Roberts, Gail L. Wrigley, Alfred A. Rabow, Graeme Walker, Christopher R. Jones, Natalie Stratton, Michael J. Waring, Rowena Callis, Lyman Feron, Robert Hugh Bradbury, Steve C. Glossop, Huawei Chen, Lara Ward, Anil Patel, Gilles Ouvry, Scott G. Lamont
Publikováno v:
Journal of Medicinal Chemistry. 59:7801-7817
Here we report the discovery and optimization of a series of bivalent bromodomain and extraterminal inhibitors. Starting with the observation of BRD4 activity of compounds from a previous program, the compounds were optimized for BRD4 potency and phy
Autor:
Graeme Walker, Tim Ikeda, Amalia Paunovic, Rowena Callis, Carly Simpson, Karen Roberts, Nick Turton, Eric Tang
Publikováno v:
SLAS Technology. 21:76-89
Since the adoption of Labcyte Echo Acoustic Droplet Ejection (ADE) technology by AstraZeneca in 2005, ADE has become the preferred method for compound dosing into both biochemical and cell-based assays across AstraZeneca research and development glob
Autor:
Anne Marie Mazzola, Graham Richmond, Craig S. Donald, Rachel Rowlinson, Celina M. D'Cruz, Michael Hulse, Camila de Almeida, Gareth M. Davies, Zena Wilson, David M. Andrews, Peter Ballard, Gordon S. Currie, Hazel M. Weir, Rowena Callis, Robert Hugh Bradbury, Jon Curwen, Mandy Lawson, Richard A. Norman, David Buttar, Ermira Pazolli, Chris De Savi, Brendon Ladd, Steve Powell, Alfred A. Rabow, Graeme Walker, Michael Tonge
Publikováno v:
Cancer Research. 75:DDT01-03
With over 70% of breast cancers expressing estrogen receptor alpha protein (ERα), treatment with either anti-hormonal therapies that directly block ERα function (e.g. tamoxifen) or therapies that block the production of estrogen itself (e.g. anastr
Autor:
Craig S. Donald, Galith Karoutchi, Syeed Hussain, Peter Ballard, Gordon S. Currie, Barry R. Hayter, Hazel M. Weir, H. Gingell, Richard A. Norman, Steven C. Glossop, David Buttar, Lyman Feron, Zena Wilson, Stuart E. Pearson, Camila de Almeida, Christopher D. Davies, Rowena Callis, Philip A. MacFaul, Thomas A. Moss, Chris De Savi, Alfred A. Rabow, David M. Andrews, Graeme Walker, Michael Tonge, Scott G. Lamont, Jon Curwen, Robert Hugh Bradbury
Publikováno v:
Journal of Medicinal Chemistry. 58:8128-8140
The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described. A directed screen identified the 1-aryl-2,3,4,9-tetrahyd
Autor:
Rowena Callis, Alfred A. Rabow, Graeme Walker, Michael Tonge, Karen Jones, Mairi Challinor, Robert Hugh Bradbury, Karen Roberts
Publikováno v:
SLAS Discovery. 20:748-759
Here, we describe an approach to identify novel selective estrogen receptor downregulator (SERD) compounds with improved properties such as oral bioavailability and the potential of increased efficacy compared to currently marketed drug treatments. P
Autor:
Sébastien L. Degorce, Patrick Ple, Mickaël Maudet, Jennifer H. Pink, Rowena Callis, Andrew Bailey, Bryan Roberts, Chris De Savi, Richard A. Norman, Rémy Morgentin, Aurélien Péru, Richard Ducray, Scott W. Martin, James S. Scott, Gillian M. Lamont, Philip A. MacFaul
Publikováno v:
Journal of Medicinal Chemistry. 58:3522-3533
A novel estrogen receptor down-regulator, 7-hydroxycoumarin (5, SS5020), has been reported with antitumor effects against chemically induced mammary tumors. Here, we report on our own investigation of 7-hydroxycoumarins as potential selective estroge
Autor:
Zena Wilson, Jon Curwen, Ermira Pazolli, Michael Hulse, N Reavey, Graeme Walker, Rachel Schiff, A.A. Rabow, Mandy Lawson, Rob H. Bradbury, Steve Powell, Agostina Nardone, Rachel Rowlinson, Celina M. D'Cruz, C. De Savi, Rowena Callis, Hazel M. Weir
Publikováno v:
Cancer Research. 73:P5-09
With over 70% of breast cancers expressing the estrogen receptor alpha (ERa), treatment with either anti-hormonal therapies that directly block ER function (e.g.Tamoxifen) or therapies that block the production of estrogen itself (e.g. aromatase inhi