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Publications
2012 publications
Andrews, M. J. I.; Clasea, J. A.; Bara, G.; Tricaricoa, G.; Edwards, P. J.; Brys, R.; Chambers, M.; Schmidt, W.; MacLeod, A.; Hirst, K.; Allen, V.; Birault, V.; Le, J.; Harris, J.; Self, A.; Nash, K.; Dixon, G. Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis. Bioorganic & Medicinal Chemistry Letters. 2012 Volume 22, Issue 6, 2266–2270.
Ahrens, T.; Bergner, A.; Sheppard, D.; Hafenbradl, D. Efficient Hit-Finding Approaches for Histone Methyltransferases: The Key Parameters. Journal of Biomolecular Screening. 2012 Volume 17 Number 1, 85-98.
2011 publications
Pollack, S. J.; Beyer, K. S.; Lock, C.; Müller, I.; Sheppard, D.; Lipkin, M.; Hardick, D.; Blurton, P.; Leonard, P. M.; Hubbard, P. A.; Todd, D.; Richardson, C. M.; Aherns, T.; Baader, M.; Hafenbradl, D. O.; Hilyard, K.; Bürli, R. W. A Comparative Study of Fragment Screening Methods on the p38 alpha Kinase: New Methods, New Insights. J. Comput Aided Mol Des. 2011. Volume 25, Number 7, 677-687.
Müller, I.; Lamers, M, B, A, C.; Ritchie, A. J.; Park, H.; Dominguez, C.; Munoz-Sanjuan, I.; Maillard, M.; Kiselyov, A. A New Apo-Caspase-6 Crystal Form Reveals the Active Conformation of the Apoenzyme. J. Mol. Biol. 2011, 410, 307-315.
Müller, I.; Lamers, M B A C.; Ritchie, AJ.; Dominguez, C.; Munoz-Sanjuan, I.; Kiselyov, A. Structure of human caspase-6 in complex with Z-VAD-FMK: New peptide binding mode observed for the non-canonical caspase conformation. Bioorganic & Medicinal Chemistry Letters. 2011, 5244-5247.
Harris, C. J.; Hill, R. D.; Sheppard, D. W.; Slater, M. J.; Stouten, P. F. W. The Design and Application of Target-Focused Compound Libraries. Combinatorial Chemistry & High Throughput Screening Volume. 2011. 14 Issue 6 pp.521-531.
Saunders, P.; Young, S.; Sander, J.; Kabelis, B.; Aullivan, A.; Evans, M.;, Clark, J.; Wilmot, J.; Hu, X.; Roberts, E.; Powell, M.; Miguel, R. N.; Furmaniak, J.; Smith, B. R. Crystal Structure of the TSH receptor (TSHR) Bound to a Blocking-Type TSHR Autoantibody. J Mol Endocrinol. 2011. Feb 15;46(2): 81-99.
This paper was prepared from research carried out by FIRS Laboratories, RSR Ltd in Cardiff, UK. It acknowledges the work carried out at BioFocus.
Kehler, J.; Ritzen, A.; Langgård, M.; Leth Peterson, S.; Farah, M M.; Bundgaard, C.; Tornby Christofferson, C T.; Nielson, J.; Paul Kilburn, J. Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors. Bioorganc & Medicinal Chemistry Letters. 2011. 21, 3738-3742.
This paper was prepared from research carried out by H. Lundbeck A/S and University of Malaya, Malaysia. It acknowledges the work carried out at BioFocus.
Hilyard, K. Epigenetics - the social network of our genes. Nature Reviews Drug Discovery. March, 2011. Volume 10, Number 3.
Hafenbradl, D.; Baumann, M.; Neumann, L. In vitro Characterization of Small-Molecule Kinase Inhibitors. Protein Kinases as Drug Targets. Wiley-VCH, 2011.
2010 publications
Burli, R.; Thomas, E.; Beaumont, V. The Role of Histone Deacetylases in Neurodegenerative Diseases and Small-Molecule Inhibitors as a Potential Therapeutics Approach. Neurodegenerative Diseases. Wiley-VCH, 2010.
Rossi, S. L.; Nistor, G.; Wyatt, T.; Yin, H. Z.; Poole, A. J.; Weiss, J. H.; Gardener, M. J.; Dijkstra, S.; Fischer, D. F.; Keirstead, H. S. Histological and Functional Benefit Following Transplantation of Motor Neuron Progenitors to the Injured Rat Spinal Cord. PLoS ONE. 2010, 5(7):e11852. doi:10.1371/journal.pone.0011852
Bürli, R. W.; Haughan, A. F.; Hodges, A. J. Development of small-molecule therapies for autoimmune diseases. Autoimmunity. 2010, Nov; 43(7) 526-538.
Newton, C. G. Where Chemists Go After Big Pharma. Chemical & Engineering News. May 31, 2010. Volume 88, Number 22. 34 - 36.
Hilyard, K. The wonderland of hit finding. Nature Reviews Drug Discovery. April, 2010. Volume 9, Number 4.
Doudou, S.; Sharma, R.; Henchman, R. H.; Sheppard, D. W.; Burton, N. A. Inhibitors of PIM-1 Kinase: A Computational Analysis of the Binding Free Energies of a Range of Imidazo [1,2-b] Pyridazines. J. Chem. Inf. Model., 2010, 50 (3), 368–379
Nash, J.; Beresford, A.; Yates, D. Intelligent ADME Outsourcing. European Pharmaceutical Review. January 2010. 20-24.
2009 publications
de Pril, R.; Perera, T.; Lekkerkerker, A. A high-content screen for inhibitors of cell migration in cancer metastasis using adenoviral knock-down. Biotech International. 2009, April/May.
Southan, A.; Clark, G. Recent advances in electrophysiology based screening technology and the impact upon ion channel discovery research. In High throughput screening: Humana press, 2009
Harris, J. Letting the target determine your compound acquisition strategy. Drug Discovery World. 2009, Spring.
Thathiah, A.; Spittaels, K.; Hoffmann, M.; Staes, M.; Cohen, A.; Horré, K.; Vanbrabant, M.; Coun, F.; Baekelandt, V.; Delecourte, A.; Fischer, D. F.; Pollet, D.; De Strooper, B.; Merchiers, P. The orphan G protein coupled receptor 3 modulates amyloid-beta peptide generation in neurons. Science. 2009, 323 (5916), 946-951
Rippmann, J. F.; Schoelch, C.; Nolte, T.; Pavliska, H.; van Marle, A,; van Es, H.; Prestle, J. Improved lipid profile through liver-specific knockdown of liver X receptor alpha in KKAy diabetic mice. J Lipid Res. 2009, 50(1) 22-31
2008 publications
Hilyard, K. Accelerating Drug Discovery. Nature Reviews Drug Discovery. 2008, volume 7, number 2.
Agüero, F.; Al-Lazikani, B.; Aslett, M.; Berriman, M.; Buckner, FS.; Campbell, R. K.; Carmona, S.; Carruthers, I. M.; Chan, A. W.; Chen, F.; Crowther, G. J.; Doyle, M. A.; Hertz-Fowler, C.; Hopkins, A. L.; McAllister, G.; Nwaka, S.; Overington, J. P.; Pain, A.; Paolini, G. V.; Pieper, U.; Ralph, S. A.; Riechers, A.; Roos, D. S.; Sali, A.; Shanmugam, D.; Suzuki, T.; Van Voorhis, W. C.; Verlinde, C. L. Genomic-scale prioritization of drug targets: the TDR Targets database. Nat Rev Drug Discovery. 2008, 7(11), 900-7.
Joesch, C.; Guevarra, E.; Parel, S. P.; Bergner, A.; Zbinden, P.; Konrad, D.; Albrecht, H. Use of FLIPR Membrane Potential Dyes for Validation of High-Throughput Screening with the FLIPR and µARCS Technologies: Identification of Ion Channel Modulators Acting on the GABAA Receptor. J. Biomol. Screening. 2008, 13(3), 218-228.
Glaser, V. Picture Im-Perfect - by expecting less, pharma can get more out of modelling. BioIT World. 2008, October.
Lease, T.; Stock, M. Compound Management: The Next Focus for Outsourcing. Pharma. 2008, Sept/Oct.
Segall, M. Send for the Software Specialists. Pharmaceutical Executive Europe. August 2008.
Lipkin, M. J.; Stevens, A P.; Livingstone, D. J.; Harris, C J.. How large does a compound screening collection need to be? Combinatorial Chemistry & High Throughput Screening. 2008, 11, 482-493.
Obrezanova, O.; Gola, J. M. R.; Champness, E.; Segall, M. Automatic QSAR modeling of ADME properties: blood-brain barrier penetration and aqueous solubility. J Comp Aid Mol Design 2008, 22(6-7) 431-40.
Segall, M. Why is it still drug discovery? European BioPharmaceutical Review. 2008 Spring.
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