Zobrazeno 1 - 10
of 81
pro vyhledávání: '"G Wynne Aherne"'
Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.
Autor:
M Cris Silva-Santisteban, Isaac M Westwood, Kathy Boxall, Nathan Brown, Sam Peacock, Craig McAndrew, Elaine Barrie, Meirion Richards, Amin Mirza, Antony W Oliver, Rosemary Burke, Swen Hoelder, Keith Jones, G Wynne Aherne, Julian Blagg, Ian Collins, Michelle D Garrett, Rob L M van Montfort
Publikováno v:
PLoS ONE, Vol 8, Iss 6, p e65689 (2013)
Checkpoint kinase 2 (CHK2) is an important serine/threonine kinase in the cellular response to DNA damage. A fragment-based screening campaign using a combination of a high-concentration AlphaScreen™ kinase assay and a biophysical thermal shift ass
Externí odkaz:
https://doaj.org/article/d0694d58cc464620a9a172b566b0062e
Autor:
Simon R Stockwell, Georgina Platt, S Elaine Barrie, Georgia Zoumpoulidou, Robert H Te Poele, G Wynne Aherne, Stuart C Wilson, Peter Sheldrake, Edward McDonald, Mathilde Venet, Christelle Soudy, Frédéric Elustondo, Laurent Rigoreau, Julian Blagg, Paul Workman, Michelle D Garrett, Sibylle Mittnacht
Publikováno v:
PLoS ONE, Vol 7, Iss 1, p e28568 (2012)
Human cancers often contain genetic alterations that disable G1/S checkpoint control and loss of this checkpoint is thought to critically contribute to cancer generation by permitting inappropriate proliferation and distorting fate-driven cell cycle
Externí odkaz:
https://doaj.org/article/921c0f22c6cd45cb99c4eb1f472162a4
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 79K, Supplementary Table 3 - Mouse body weights for data in Figure 4A Body Weights expressed as a percentage of the weight on day 0 for mice bearing HT29 xenografts and treated with gemcitabine (100mg/kg iv), CCT244747 (75mg/kg po) or the c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::401ea57b719c1a1d93ab5881aa5484ab
https://doi.org/10.1158/1078-0432.22445615
https://doi.org/10.1158/1078-0432.22445615
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 92K, Supplementary Figure 2. A constrained, scaffold docking model of CCT244747 in the ATP pocket of human CHK1 realized using the SAR-020106 X-ray crystal structure (PDB 2ym8).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9db6fcbdeb80531e3ddd7d42e0cafbdd
https://doi.org/10.1158/1078-0432.22445639
https://doi.org/10.1158/1078-0432.22445639
Autor:
Michelle D. Garrett, Ian Collins, John C. Reader, David H. Williams, Florence I. Raynaud, Suzanne A. Eccles, G. Wynne Aherne, Kathy J. Boxall, Gary Box, Alexis De Haven Brandon, Melanie Valenti, Angela Hayes, Paul D. Eve, Michael I. Walton
PDF file, 63KB, Kinase inhibitory profile of SAR-020106 at 10 μMa.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32afb33095afaa0235fcca7f9841e0bf
https://doi.org/10.1158/1535-7163.22485369
https://doi.org/10.1158/1535-7163.22485369
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 118K, Supplementary Table 2 Summary of Effects of Irinotecan, Gemcitabine and CCT244747 alone or in combination on human tumor xenografts growth delay.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d1bd0e4da26aa07abae832d484513eb
https://doi.org/10.1158/1078-0432.22445618
https://doi.org/10.1158/1078-0432.22445618
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 810K, Supplementary Figure 3 Characterisation of the effects of minimally toxic concentrations of CCT244747 alone or in combination with genotoxic agents (+) in HT29 and SW620 colon cancer cell lines. A, HT29 cells were treated with SN38 (1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::343131448e94d2702194f9a5362972e1
https://doi.org/10.1158/1078-0432.22445636
https://doi.org/10.1158/1078-0432.22445636
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 67K, Supplementary Figure 4. Effects of scheduling and exposure times on the ability of two different CHK1 inhibitors to potentiate gemcitabine cytotoxicity in SW620 cells in vitro. A, Effect of different contact times on the capacity of SA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::645f855fb751a0d3f4a65c2278c348bf
https://doi.org/10.1158/1078-0432.22445633.v1
https://doi.org/10.1158/1078-0432.22445633.v1
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 36K, Supplementary Figure 5. Effects of acute CCT244747 administration on non-tumor bearing GEMM mouse body weights. CCT244747 was administered at a dose of 150mg/kg p.o. x 7days and mouse body weights were measured daily. Results are mean
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9d8453adbf17f84bf89f67ba5ef474c
https://doi.org/10.1158/1078-0432.22445630
https://doi.org/10.1158/1078-0432.22445630
Autor:
Michelle D. Garrett, Ian Collins, Suzanne A. Eccles, Florence I. Raynaud, Louis Chesler, John C. Reader, G. Wynne Aherne, Simon P. Robinson, Yann Jamin, Thomas P. Matthews, Michael Lainchbury, Kathy J. Boxall, Elizabeth L. Smith, Albert Hallsworth, Gary Box, Alexis K. De Haven Brandon, Melanie R. Valenti, Angela Hayes, Paul D. Eve, Mike I. Walton
PDF file, 76K, Supplementary Table 1 Kinome selectivity profile of CCT244747 CCT244747 was tested at 1 μM (140 enzymes) and 10 μM (121 enzymes) for inhibition of human kinases in a radiometric protein phosphorylation assay (MRC Protein Phosphorylat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbea4bf2cbee88a83459a4ad37108cee
https://doi.org/10.1158/1078-0432.22445621.v1
https://doi.org/10.1158/1078-0432.22445621.v1