Πλοήγηση ανά Συγγραφέα "Mezna, M."
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Catch the kinase conformer
McInnes, C.; Mezna, M.; Kontopidis, G. (2006)Protein kinases exist in inactive and active states, but little attention has been paid to which state is or should be the target in drug discovery efforts. In this issue of Chemistry & Biology, Okram et al. [1] tackle ... -
Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents
Wang, S.; Griffiths, G.; Midgley, C. A.; Barnett, A. L.; Cooper, M.; Grabarek, J.; Ingram, L.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; McLachlan, J.; Meades, C.; Mezna, M.; Stuart, I.; Thomas, M. P.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Blake, D. G.; Fischer, P. M. (2010)The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity, since the ATP-binding motif is present in many proteins. We introduce a strategy that has allowed us to identify compounds ... -
Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors
Wang, S.; Midgley, C. A.; Scaërou, F.; Grabarek, J. B.; Griffiths, G.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; Meades, C.; Mezna, M.; Plater, A.; Stuart, I.; Thomas, M. P.; Wood, G.; Clarke, R. G.; Blake, D. G.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Fischer, P. M. (2010)Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic ... -
Targeting active and inactive CDK2 differential binding inhibitors
Kontopidis, G.; McInnes, C.; Pandalaneni, S.; McNae, I.; Gibson, D.; Mezna, M.; Thomas, M.; Wood, G.; Wang, S.; Walkinshaw, M.; Fischer, P. (2008)