Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Stuart E. Pearson"'
Autor:
Chris De Savi, Celina D'Cruz, Anne Marie Mazzola, Ermira Pazolli, Brendon Ladd, Graham Richmond, Claire Sadler, Steve Powell, Rachel Rowlinson, Zena Wilson, Graeme E. Walker, Gareth Davies, Michael Tonge, Stuart E. Pearson, Richard A. Norman, Thomas Moss, Philip MacFaul, Galith Karoutchi, Lyman J.L. Feron, Craig S. Donald, Michael Hulse, Peter Ballard, Camila de Almeida, Jon O. Curwen, Rowena J. Callis, David Buttar, Alfred A. Rabow, Mandy Lawson, Robert H. Bradbury, Hazel M. Weir
Legends for Supplementary Figures 1 - 7.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f2ea8b1988f522a97b4476bc1bfb489
https://doi.org/10.1158/0008-5472.22409537.v1
https://doi.org/10.1158/0008-5472.22409537.v1
Autor:
Chris De Savi, Celina D'Cruz, Anne Marie Mazzola, Ermira Pazolli, Brendon Ladd, Graham Richmond, Claire Sadler, Steve Powell, Rachel Rowlinson, Zena Wilson, Graeme E. Walker, Gareth Davies, Michael Tonge, Stuart E. Pearson, Richard A. Norman, Thomas Moss, Philip MacFaul, Galith Karoutchi, Lyman J.L. Feron, Craig S. Donald, Michael Hulse, Peter Ballard, Camila de Almeida, Jon O. Curwen, Rowena J. Callis, David Buttar, Alfred A. Rabow, Mandy Lawson, Robert H. Bradbury, Hazel M. Weir
Supplementary Figure 1 contains a Western blot showing the amount of estrogen receptor remaining after treatment of MCF-7 cells with AZD9496, fulvestrant and estradiol alongside GAPDH protein levels as an internal gel loading control; Supplementary F
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14c5919450d0037769dc8885c171e5d8
https://doi.org/10.1158/0008-5472.22409534.v1
https://doi.org/10.1158/0008-5472.22409534.v1
Autor:
Chris De Savi, Celina D'Cruz, Anne Marie Mazzola, Ermira Pazolli, Brendon Ladd, Graham Richmond, Claire Sadler, Steve Powell, Rachel Rowlinson, Zena Wilson, Graeme E. Walker, Gareth Davies, Michael Tonge, Stuart E. Pearson, Richard A. Norman, Thomas Moss, Philip MacFaul, Galith Karoutchi, Lyman J.L. Feron, Craig S. Donald, Michael Hulse, Peter Ballard, Camila de Almeida, Jon O. Curwen, Rowena J. Callis, David Buttar, Alfred A. Rabow, Mandy Lawson, Robert H. Bradbury, Hazel M. Weir
Fulvestrant is an estrogen receptor (ER) antagonist administered to breast cancer patients by monthly intramuscular injection. Given its present limitations of dosing and route of administration, a more flexible orally available compound has been sou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::121cf8596ca6963e592f8c1559e47fd8
https://doi.org/10.1158/0008-5472.c.6507809.v1
https://doi.org/10.1158/0008-5472.c.6507809.v1
Autor:
Chris De Savi, Celina D'Cruz, Anne Marie Mazzola, Ermira Pazolli, Brendon Ladd, Graham Richmond, Claire Sadler, Steve Powell, Rachel Rowlinson, Zena Wilson, Graeme E. Walker, Gareth Davies, Michael Tonge, Stuart E. Pearson, Richard A. Norman, Thomas Moss, Philip MacFaul, Galith Karoutchi, Lyman J.L. Feron, Craig S. Donald, Michael Hulse, Peter Ballard, Camila de Almeida, Jon O. Curwen, Rowena J. Callis, David Buttar, Alfred A. Rabow, Mandy Lawson, Robert H. Bradbury, Hazel M. Weir
Supplementary Table 1 contains crystallographic data collection and refinements statistics for AZD9496 binding to the human estrogen receptor α ligand binding domain, Supplementary Table 2 shows the rate constants for association, dissociation and e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fc4d27d54650a74388b4e3bbd209d6f
https://doi.org/10.1158/0008-5472.22409528
https://doi.org/10.1158/0008-5472.22409528
Autor:
Chris De Savi, Celina D'Cruz, Anne Marie Mazzola, Ermira Pazolli, Brendon Ladd, Graham Richmond, Claire Sadler, Steve Powell, Rachel Rowlinson, Zena Wilson, Graeme E. Walker, Gareth Davies, Michael Tonge, Stuart E. Pearson, Richard A. Norman, Thomas Moss, Philip MacFaul, Galith Karoutchi, Lyman J.L. Feron, Craig S. Donald, Michael Hulse, Peter Ballard, Camila de Almeida, Jon O. Curwen, Rowena J. Callis, David Buttar, Alfred A. Rabow, Mandy Lawson, Robert H. Bradbury, Hazel M. Weir
Methods are given for: the use of SILAC assays to measure the rate of estrogen receptor α peptide degradation over time, the measurement of compound binding affinity of estrogen receptor α ligand binding domain using BIAcore, immunoblotting of estr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::500fb6b45ef15b3a4c16d2efaec374bf
https://doi.org/10.1158/0008-5472.22409531
https://doi.org/10.1158/0008-5472.22409531
Autor:
James M. Smith, Rana Anjum, Sébastien L. Degorce, Ina Terstiege, Turner Paul, Stuart E. Pearson, Michael J. Tucker, Alexandra L. Orton, Charlene Fallan, Graeme Scarfe, Anna Aagaard, James S. Scott, Oliver R. Steward, Yafeng Xue, Iain A. Cumming, Tony Johnson, Gail L. Wrigley, Karl-Johan Leuchowius, Stephen D. Wilkinson, Graeme R. Robb, Coura R. Diène, Alan Rosen
Publikováno v:
Bioorganicmedicinal chemistry. 28(23)
In this article, we report our efforts towards improving in vitro human clearance in a series of 5-azaquinazolines through a series of C4 truncations and C2 expansions. Extensive DMPK studies enabled us to tackle high Aldehyde Oxidase (AO) metabolism
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15d8595e2345eb1625eb48d9c502e86b
https://pubmed.ncbi.nlm.nih.gov/33091850
https://pubmed.ncbi.nlm.nih.gov/33091850
Autor:
Darren Stead, Michael J. Tucker, Steve Stokes, Martin J. Packer, Christopher Hardy, Ross Overman, Scott Boyd, Stuart E. Pearson, Deepa Bhavsar, Andrew D. Campbell, Derek Ogg, Michael Grondine, Sylvie Guichard, Evan Barry, Marianne Schimpl, James M. Smith, Yang Ye, Kristin Goldberg, Thomas Anthony Hunt, Aaron Smith, Crystal Brown, Jason Grant Kettle, Wenlin Shao, Olga Moleva, Rana Anjum, Xiuwei Li, Rhys D.O. Jones
Publikováno v:
Journal of Medicinal Chemistry. 61:8797-8810
While the treatment of gastrointestinal stromal tumors (GISTs) has been revolutionized by the application of targeted tyrosine kinase inhibitors capable of inhibiting KIT-driven proliferation, diverse mutations to this kinase drive resistance to esta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91c6c2cf07988c6c4bbfe6872729c481
https://doi.org/10.1021/acs.jmedchem.8b00938
https://doi.org/10.1021/acs.jmedchem.8b00938
Autor:
Stuart E. Pearson, Kristin Goldberg, Jonathan E. Finlayson, Anil Patel, Shaun M. Fillery, Jonathan M. Eden, Julie Demeritt
Publikováno v:
Synthesis. 50:4963-4981
Isoquinolines activated with sulfamoyl chlorides were reacted with indoles in a 3-component reaction to generate a library of dihydroisoquinoline derivatives. Using a differential protecting group strategy, products could be further derivatised. Synt
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::53eb0ff59b4ac9bd7a3a9f4820d316c0
https://doi.org/10.1055/s-0037-1610223
https://doi.org/10.1055/s-0037-1610223
Autor:
Allan Dishington, Guohong Xin, Nicola Colclough, Stephen T. Durant, Anil Patel, Stuart E. Pearson, Lorraine A. Hassall, Kurt Gordon Pike, Kristin Goldberg, Thomas M. McGuire, Andrew D. Campbell, Baochang Zhai, Jens Petersen, Gareth Hughes, Elaine Cadogan, Barlaam Bernard Christophe, Natalie Stratton, Graeme R. Robb, Martin Pass, Philip A. MacFaul
[Image: see text] We report the discovery of a novel series of 3-cinnoline carboxamides as highly potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitors. Optimization of this series focusing on potency and physicochemical properti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7819cdd683c89fe377bbcb34c1ebbca2
https://europepmc.org/articles/PMC6088353/
https://europepmc.org/articles/PMC6088353/
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a9d21c50ca9de0e32e23964631039a67
https://doi.org/10.1021/acs.jmedchem.5b00984
https://doi.org/10.1021/acs.jmedchem.5b00984