Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Andrew Cansfield"'
Autor:
Gavin Bennett, Anne J. Rüger, John Thomas Feutrill, Rosemary Lynch, Ann Lewis, Anthea L. Newton, Nico Zinn, Tammy Ladduwahetty, Sunose Mihiro, Andrew Cansfield, Giovanna Bergamini, Oliver Rausch, Alan P. Watt, Douglas W. Thomson, Katie Ellard
Publikováno v:
ACS Medicinal Chemistry Letters. 7:768-773
CZ415, a potent ATP-competitive mTOR inhibitor with unprecedented selectivity over any other kinase is described. In addition to a comprehensive characterization of its activities in vitro, in vitro ADME, and in vivo pharmacokinetic data are reported
Autor:
Allan E. Surgenor, James B. Murray, Alan Robertson, Martin J. Parratt, Andrew Cansfield, Christopher J. Torrance, Pawel Dokurno, Jenifer Borgognoni, Jonathan D. Moore, Christine M. Richardson, Douglas S. Williamson, Geraint L. Francis, Rob Howes
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1353-1357
Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen s
Autor:
Warren Miller, Giovanna Bergamini, Mihiro Sunose, Jess Taylor, Gitte Neubauer, Andrew Cansfield, Nigel Ramsden, Katie Ellard, Kathryn Bell
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(16)
Herein we describe the SAR of a novel series of 6-aryl-2-amino-triazolopyridines as potent and selective PI3Kγ inhibitors. The 6-aryl-triazolopyridine core was identified by chemoproteomic screening of a kinase focused library. Rapid chemical expans
Autor:
Katie Ellard, Marcus Bantscheff, Satoko Shimamura, Kathryn Bell, Carsten Hopf, Faiza Rharbaoui, Nigel Ramsden, Mikhail M. Savitski, Gerard Drewes, Gitte Neubauer, Raffaella Mangano, Andrew Cansfield, Toby Mathieson, Ivan Plavec, Christina Rau, Friedrich B M Reinhard, Daniel Leggate, Alison O'Mahony, Thilo Werner, Carola Doce, Jessica Perrin, Katrin Müller, Giovanna Bergamini, Oliver Rausch, Emilio Hirsch
Publikováno v:
Nature chemical biology. 8(6)
We devised a high-throughput chemoproteomics method that enabled multiplexed screening of 16,000 compounds against native protein and lipid kinases in cell extracts. Optimization of one chemical series resulted in CZC24832, which is to our knowledge
Autor:
Sarah Denny, Andrew Cansfield, Philip Stephen Jackson, Jonathan D. Moore, Douglas S. Williamson, Peter Kierstan, Lan-Zhen Wang, Simon F. Scrace, Joanne Wayne, Andrea M. Lockie, Nicola J. Curtin, Carol Bentley, David R. Newell, Jenifer Borgognoni
Publikováno v:
Cell cycle (Georgetown, Tex.). 7(24)
Transient treatment with small molecule CDK inhibitors is toxic to cancer cells and leads to depletion of anti-apoptotic proteins and Chk1, coupled with DNA damage and induction of apoptosis. Here we have examined, which of these phenomena are necess
Autor:
Alan Robertson, Justin Bower, Andrew Cansfield, Pawel Dokurno, James B. Murray, Jonathan D. Moore, Jenifer Powles, Geraint L. Francis, Richard Hebdon, Martin J. Parratt, Andrea M. Lockie, Douglas S. Williamson, Philip Stephen Jackson, Allan E. Surgenor, Christopher J. Torrance, Claire L. Nunns, Christine M. Richardson, Rob Howes
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(4)
The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for C
Autor:
David R. Vesey, Christopher H. Hill, Rino A. Bit, Christopher J. Hobbs, Eric A. Kitas, Brad S. Sherborne, David Pole, Fiona Wilson, Antonin Kroehn, Glyn Williams, Bill Harris, Ian R. Kilford, David Banner, Neera Borkakoti, D.Lee Walmsley, David Whittaker, Paul Rugman, Andrew Cansfield, Ian Edward David Smith, Allan Surgenor, Katherine L. Hilyard, Peter Lovell
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(10)
Starting from the tetrapeptide Ac-pYEEI-NHMe and using a structure-based approach, we have designed and synthesised a peptidomimetic ligand for p56(lck) SH2 domain containing a conformationally restricted replacement for the two glutamate residues. W
Autor:
Carola Doce, Friedrich B M Reinhard, Thilo Werner, Raffaella Mangano, Satoko Shimamura, Katrin Müller, Nigel Ramsden, Gerard Drewes, Daniel Leggate, Gitte Neubauer, Jessica Perrin, Toby Mathieson, Alison O'Mahony, Marcus Bantscheff, Andrew Cansfield, Faiza Rharbaoui, Kathryn Bell, Carsten Hopf, Oliver Rausch, Mikhail M. Savitski, Ivan Plavec, Christina Rau, Katie Ellard, Giovanna Bergamini, Emilio Hirsch
Publikováno v:
Nature Chemical Biology. 8:737-737
Nat. Chem. Biol. 8, 576–582 (2012); published online 29 April 2012; corrected after print 16 May 2012 In the version of this article initially published, the name M. Sunose was misspelled in the Acknowledgements. The error has been corrected in the