Publications

2011 publications

Ahrens, T.; Bergner, A.; Sheppard, D.; Hafenbradl, D.  Efficient Hit-Finding Approaches for Histone Methyltransferases: The Key Parameters. Journal of Biomolecular Screening.  2011, doi: 10.1177/1087057111422823

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 aknowledges 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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