Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Galith Karoutchi"'
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:
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
Autor:
Andrew David Morley, Galith Karoutchi, Stefan Gerhardt, Attilla Ting, Chris De Savi, Nash Ian Alun, Ken Page
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:271-277
Directed screening has identified a novel series of non-zinc binding MMP13 inhibitors that possess good levels of activity whilst demonstrating excellent selectivity over related MMPs. A lead optimisation campaign has delivered compounds with enhance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1edcdff0979b6502875d67bc0caf41a9
https://doi.org/10.1016/j.bmcl.2011.11.034
https://doi.org/10.1016/j.bmcl.2011.11.034
Autor:
Michael James, Gordon A. Hamlin, Stefan Gerhardt, David Ryan, Nash Ian Alun, Attilla Ting, Stephen J. Norris, Galith Karoutchi, Chris De Savi, Neil Rankine, David J. Hargreaves, Christine M. Wood, Sarah V. Baker, Philip A. MacFaul, Andrew David Morley, Kostas Karabelas
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4215-4219
Directed screening has identified a novel series of MMP13 inhibitors that possess good levels of activity whilst possessing excellent selectivity over related MMPs. The binding mode of the series has been solved by co-crystallisation and demonstrates
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::edfdcf46848c274f3946020e4941981e
https://doi.org/10.1016/j.bmcl.2011.05.075
https://doi.org/10.1016/j.bmcl.2011.05.075
Autor:
Stefan Gerhardt, Andrew David Morley, Peter W. Kenny, Hannes Simader, Emma V. Jones, Galith Karoutchi, Stephan Krapp, Neil Rankine, Keith Oldham, Paul A. Bethel, Stefan Steinbacher, Martin Augustin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4622-4625
A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b5e987a8e0f4a810fd0d5bfae2d2508
https://doi.org/10.1016/j.bmcl.2009.06.090
https://doi.org/10.1016/j.bmcl.2009.06.090
Autor:
Neil Rankine, Linda J. Wood, Galith Karoutchi, Michelle Coulson, Keith Oldham, Emma V. Jones, Paul A. Bethel, Stephan Krapp, Susannah J. Ford, Stefan Gerhardt, David Ryan, Matthew Grist, Peter W. Kenny, Hannes Simader, Andrew David Morley, Stuart L. Wells, Gordon A. Hamlin, Stefan Steinbacher, Jack E. Dawson, Nabil Asaad, Martin Augustin, Michael James
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4280-4283
A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca39a993160acd7584b90a963ada1ade
https://doi.org/10.1016/j.bmcl.2009.05.071
https://doi.org/10.1016/j.bmcl.2009.05.071