News & Events - Publications

Sareum scientists have over 200 years drug discovery experience, selected publications include;

Identification and Structure-guided Optimisation of Novel Inhibitors of Checkpoint Kinase 1 (Chk1) through Combined Biochemical and Crystallographic Screening. Reader, J., Williams, D., Klair, S., Cherry, M., Fisher, M., Scanlon, J., Piton, N., Addison, G., Lamers, M., et al. AACR Annual Meeting, San Diego, CA, Apr 12-16, 2008. Download PDF
Finding protein kinase hits using structural information. Cherry, M., Reader, J. and Williams, D.H. Prog. Med. Chem., (2006). 44, 1-63.
Fragment-Based Drug Design, Mitchell, T. and Cherry, M. Innovations in Pharmaceutical Technology, (2005). 16, 34-36. Download PDF
The design of a new potent and selective ligand for the BRS3 receptor. Boyle, R.G., Humphries, J., Mitchell, T., Showell, G.A., Iijima, H., Shimada, H., Arai, T., Ueno, H., Usui, H., Sakaki, T., Wada, E. and Wada, K. J Peptide Research, (2005). 11(3), 136-141.
Recent kinase and kinase inhibitor x-ray structures: Mechanisms of inhibition and selectivity insights. Cherry, M. and Williams, D. H. Current Medicinal Chemistry, (2004). 11, 663-673.
Automation in medicinal chemistry. Reader, John C. Current Topics in Medicinal Chemistry, (2004), 4(7), 671-686.
ACE2 structures reveal a large hinge-bending motion important for inhibitor binding and catalysis. Towler, P., Staker, B., Prasad, S.G., Menon, S., Tang, J., Parsons, T., Ryan, D., Fisher, M., Williams, D.H., Dales, N.A., Patane, M.A. and Pantoliano, M.W. J. Biol. Chem., (2004). 279, 17996 - 18007.
Solid phase synthesis of tetrahydro-1,4-benzodiazepin-2-ones. Hone, Neal D.; Wilson, William; Reader, John C. Tetrahedron Letters, (2003). 44(46), 8493-8495.
Solid-phase synthesis of dibenzoxazepinones. Hone, Neal D., Salter, James I., Reader, John C. Tetrahedron Letters, (2003). 44(44), 8169-8172.
Reusable resin plug-bound palladium catalysts for organic synthesis. Atrash, B., Reader, J. and Bradley, M. Tetrahedron Letters, (2003). 44(25), 4779-4782.
Descriptors, Physical Properties and Drug-Likedness. Brüstle, M., Beck, B., Schindler, T., King, W., Mitchell, T. and T. Clark, T. J. Med. Chem., (2002). 45(16), 3345-3355.
Latest developments in crystallography and structure-based design of protein kinase inhibitors as drug candidates. Williams, D.H. and Mitchell T. Curr Opin. Pharmacology, (2002). 2, 567-573.
Structure of a Cys25 to Ser Mutant of human cathepsin S. Turkenburg, J.P, Lamers, M.B.A.C., Brzozowski, M.A., Wright, L.M., Hubbard, R.E., Sturt, S.L., and Williams, D.H. Acta Cryst D (Biological Crystallography), (2002). 58, 451-455.
Design, Synthesis, and Biological Evaluation of a Library of 1-(2-Thiazolyl)-5-(trifluoromethyl)pyrazole-4-carboxamides. Donohue, B.A., Michelotti, E.L., Reader, J.C., Reader, V., Stirling, M. and Tice, C.M. Journal of Combinatorial Chemistry, (2002). 4(1), 23-32.
Design Strategies for building drug-like chemical libraries. Mitchell, T. & Showell, G. Curr. Opin. Drug Disc. Dev., (2001). 4(3), 314-318.
Baculoviral Expression and Characterisation of Rodent Cathepsin S. Mason, C.S., Lamers, M.B.A.C., Henderson, I, Monk, T. and Williams, D.H. Protein Exp. Purif., (2001). 23, 45-54.
Revolutionizing resin handling for combinatorial synthesis. Atrash, B., Bradley, M., Kobylecki, R., Cowell, D. and Reader, J. Angewandte Chemie, International Edition, (2001). 40(5), 938-941.
The X-ray structure of Brassica napus beta-keto acyl carrier protein reductase and its implications for substrate binding and catalysis. Fisher, M., Kroon, J.T., Martindale, W., Stuitje, A.R., Slabas, A.R. and Rafferty, J.B. Structure Folding Des., (2000). 8(4), 339-47.
Lamers, M.B.A.C., Antson, A., Scott, R.G., Hubbard, R.E. and Williams, D.H. Structure of the Protein Tyrosine Kinase Domain of C-terminal Src Kinase (CSK) in Complex with Staurosporine. J. Mol. Biol., (1999). 285, 713-725.
Crystal Structure of the Zinc-Dependent -Lactamase from Bacillus cereus at 1.9A Resolution: Binuclear Active Site with Features of a Mononuclear Enzyme. Fabiane, S., Sohi, M., Wan, T., Payne, D., Bateson, J., Mitchell, T. & Sutton, B. Biochemistry, (1998). 37(36), 12404-12411.
The crystal structure of an intact human Max-DNA complex: new insights into mechanisms of transcriptional control. Brownlie, P., Ceska, T., Lamers, M., Romier, C., Stier, G., Teo, H. and Suck, D. Structure, (1997). 5(4), 509-520.
Structure of the catalytic domain of human fibroblast collagenase complexed with an inhibitor. Borkakoti, N., Winkler, F.K., Williams, D.H., D'Arcy, A., Broadhurst, M.J., Brown P.A., Johnson, W.H. and Murray, E.J. Nature Structural Biology, (1994). 1(2), 106-110.
The X-ray structure of an atypical homeodomain present in the rat liver transcription factor LFB1/HNF1 and implications for DNA binding. Ceska, T, A., Lamers, M., Monaci, P., Nicosia, A., Cortese, R and Suck, D. EMBO J, (1993). 5, 1805-10.

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