Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Paul Brough"'
Autor:
Stephen Stokes, Patrick C. Mahon, Alan D. Robertson, Jalanie D’Alessandro, Paul Webb, Charles Parry, Lisa Baker, Natalia Matassova, Nicholas G. M. Davies, Sean McKenna, Andrew Massey, Rachel Parsons, Yikang Wang, Macias Alba, Paul Brough, Ben Davis, Michael Wood, Simon Bedford, Jonathan D. Moore, Christopher J. Northfield, Loic le Strat, Stephen D. Roughley, Daniel Maddox, Seema Chavda, James Brooke Murray, Allan E. Surgenor, Johannes W. G. Meissner, Terry Shaw, Heather Simmonite, Stefaniak Emma Jayne, Victoria Chell, Neil Whitehead, Kirsten Brown
Publikováno v:
Journal of medicinal chemistry. 60(6)
Libraries of nonpurified resorcinol amide derivatives were screened by surface plasmon resonance (SPR) to determine the binding dissociation constant (off-rate, kd) for compounds binding to the pyruvate dehydrogenase kinase (PDHK) enzyme. Parallel of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb5f231f5660155f00b4666296b0e799
https://pubmed.ncbi.nlm.nih.gov/28199108
https://pubmed.ncbi.nlm.nih.gov/28199108
Autor:
Anna Staniszewska, Lisa Baker, Jonathan D. Moore, James Murray, Patrick C. Mahon, Terence Shaw, Paul Brough, Alan Surgenor, Michael Wood, Ben Davis, Jalanie D’Alessandro, Natalia Matassova, Macias Alba
Publikováno v:
Scopus-Elsevier
Oncotarget
Oncotarget
Pyruvate dehydrogenase kinase (PDK) is a pivotal enzyme in cellular energy metabolism that has previously been implicated in cancer through both RNAi based studies and clinical correlations with poor prognosis in several cancer types. Here, we report
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66a89876a6f42b6b5319184f7f142c89
https://doi.org/10.18632/oncotarget.2656
https://doi.org/10.18632/oncotarget.2656
Autor:
Andrew Massey, Stephanie Geoffrey, Stuart C. Ray, Hart Terance William, Joseph Schoepfer, Michael Wood, Nicholas G. M. Davies, James A. H. Murray, Paul Webb, Michael Rugaard Jensen, Roderick E. Hubbard, Nicolas Foloppe, Jonathan D. Moore, Lisa Wright, Allan E. Surgenor, Robert M. Pratt, Kirsten Scriven, Alan D. Robertson, Stephen Stokes, Paul Brough, Howard Langh Am Mansell, Martin J. Drysdale, Natalia Matassova, Stephen D. Roughley, Ben Davis, Helen Browne, Heather Simmonite, Ben Gibbons
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:6770-6789
Inhibitors of the Hsp90 molecular chaperone are showing promise as anti-cancer agents. Here we describe a series of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine ATP competitive Hsp90 inhibitors that were identified following structure-driven optimization o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c5af7f4f0c7d0b734456f7d6823c0de
https://doi.org/10.1016/j.bmc.2012.08.050
https://doi.org/10.1016/j.bmc.2012.08.050
Autor:
Rob Howes, Suzanne A. Eccles, Angela Hayes, Brian Dymock, Paul Webb, Xavier Barril, Paul Brough, Andrew Massey, Melanie Valenti, Alan Surgenor, Thomas P. Matthews, Michael Wood, Wynne Aherne, Alexis De Haven Brandon, Martin J. Drysdale, Vanessa Martins, Keith Jones, Roderick E. Hubbard, Sharon Gowan, Karen James, Laurence H. Pearl, Paul Workman, Kathy Boxall, Edward McDonald, Florence I. Raynaud, Frederique Urban, Lisa Wright, Gary Box, Chrisostomos Prodromou, Martin G. Rowlands, Kwai-Ming Cheung, Swee Y. Sharp, Harry Finch, Julie E. Cansfield, F. E. Boxall, Andrew Kalusa, Lisa Patterson
Publikováno v:
Cancer Research. 68:2850-2860
We describe the biological properties of NVP-AUY922, a novel resorcinylic isoxazole amide heat shock protein 90 (HSP90) inhibitor. NVP-AUY922 potently inhibits HSP90 (Kd = 1.7 nmol/L) and proliferation of human tumor cells with GI50 values of approxi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a256218c0400cd01dde35ed49b58f8ef
https://doi.org/10.1158/0008-5472.can-07-5256
https://doi.org/10.1158/0008-5472.can-07-5256
Autor:
Karen James, Ian Collins, Kathy Boxall, Brian Dymock, Paul Workman, Florence I. Raynaud, Chrisostomos Prodromou, Angela Hayes, Suzanne A. Eccles, Kwai-Ming J. Cheung, Allan E. Surgenor, Paul Webb, Martin J. Drysdale, D. Lee Walmsley, Stuart C. Ray, Allan M. Jordan, Jenifer Borgognoni, Vanessa Martins, Swee Y. Sharp, Andrea M. Lockie, Nicholas G. M. Davies, R. Howes, Lisa Wright, Thomas P. Matthews, Andrew Massey, Michael Wood, Roderick E. Hubbard, Wynne Aherne, Stephen D. Roughley, Alexandra Fink, Harry Finch, Julie E. Cansfield, Christopher J. Northfield, Paul Brough, Edward McDonald, Xavier Barril, Laurence H. Pearl
Publikováno v:
Journal of Medicinal Chemistry. 51:196-218
Inhibitors of the Hsp90 molecular chaperone are showing considerable promise as potential chemotherapeutic agents for cancer. Here, we describe the structure-based design, synthesis, structure-activity relationships and pharmacokinetics of potent sma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1119161a7c8a6071c66a4cc2e2330e66
https://doi.org/10.1021/jm701018h
https://doi.org/10.1021/jm701018h
Publikováno v:
Current Topics in Medicinal Chemistry. 6:1193-1203
This review explains why the chaperone Hsp90 is an exciting protein target for the discovery of new drugs to treat cancer in the clinic, and summarises the properties of natural product derived inhibitors before relating the discovery and current sta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2668cd57052ff3d9f1ef7f25c382f4c
https://doi.org/10.2174/156802606777812086
https://doi.org/10.2174/156802606777812086
Autor:
Allan E. Surgenor, Andrew Massey, Lisa Wright, Paul Brough, Martin J. Drysdale, Xavier Barril, Roderick E. Hubbard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5187-5191
Docking-based virtual screening identified 1-(2-phenol)-2-naphthol compounds as a new class of Hsp90 inhibitors of low to sub-micromolar potency. Here we report the binding affinities and cellular activities of several members of this class. A high r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2439d42099ec8104de87fb8ce57fe3a5
https://doi.org/10.1016/j.bmcl.2005.08.092
https://doi.org/10.1016/j.bmcl.2005.08.092
Autor:
Martin J. Drysdale, Paul Workman, Paul Brough, Allan E. Surgenor, Mandy Beswick, Xavier Barril, Andrew Massey, Brian Dymock, K. Grant, Lisa Wright
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5197-5201
Information from X-ray crystal structures of Hsp90 inhibitors bound to the human Hsp90 molecular chaperone was used to assist in the design of 3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as novel inhibitors of Hsp90. Accessing an extra i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67d85c173513fd57092f3762541d288b
https://doi.org/10.1016/j.bmcl.2005.08.091
https://doi.org/10.1016/j.bmcl.2005.08.091
Autor:
Brian Dymock, Roderick E. Hubbard, Paul Brough, Paul Webb, Allan E. Surgenor, Edward McDonald, Paul Workman, Xavier Barril, Stephen D. Roughley, Martin J. Drysdale, Lisa Wright, Julie E. Cansfield, Andrew Massey
Publikováno v:
Journal of Medicinal Chemistry. 48:4212-4215
The crystal structure of a previously reported screening hit 1 (CCT018159) bound to the N terminal domain of molecular chaperone Hsp90 has been used to design 5-amide analogues. These exhibit enhanced potency against the target in binding and functio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d3e7208e7f3a654ab1c1bfa82e41280
https://doi.org/10.1021/jm050355z
https://doi.org/10.1021/jm050355z
Publikováno v:
Journal of medicinal chemistry. 57(7)
The dissociation rate constant kd (off-rate) is the component of ligand–protein binding with the most significant potential to enhance compound potency. Here we provide theoretical and empirical data to show that this parameter can be determined ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d98d4c6fe1af41fdd26c1368f5142e7f
https://pubmed.ncbi.nlm.nih.gov/24520903
https://pubmed.ncbi.nlm.nih.gov/24520903