Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Peter Kierstan"'
Autor:
Philip Stephen Jackson, Douglas S. Williamson, Martin J. Drysdale, Claire L. Nunns, Roderick E. Hubbard, Rob Howes, Harry Finch, Peter Kierstan, Martin J. Parratt, Jonathan D. Moore, Allan E. Surgenor, Heather Simmonite, Christopher J. Torrance, Georg Lentzen, Christine M. Richardson, Jenifer Borgognoni, Pawel Dokurno, James Brooke Murray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3880-3885
Virtual screening against a pCDK2/cyclin A crystal structure led to the identification of a potent and novel CDK2 inhibitor, which exhibited an unusual mode of interaction with the kinase binding motif. With the aid of X-ray crystallography and model
Autor:
Rob Howes, Andrew Potter, Nicolas Foloppe, Lisa M. Fisher, Peter Kierstan, Geraint L. Francis
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:1792-1804
Inhibition of the Chk1 kinase by small molecules binding to its active site is a strategy of great therapeutic interest for oncology. We report how computational modelling predicted the binding mode of ligands of special interest to the Chk1 ATP site
Autor:
Andrew Potter, Lisa M. Fisher, Nicolas Foloppe, Peter Kierstan, Allan E. Surgenor, Rob Howes, and Alan G. S. Robertson
Publikováno v:
Journal of Medicinal Chemistry. 48:4332-4345
We report the discovery, synthesis, and crystallographic binding mode of novel furanopyrimidine and pyrrolopyrimidine inhibitors of the Chk1 kinase, an oncology target. These inhibitors are synthetically tractable and inhibit Chk1 by competing for it
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