High-throughput hit finding and compound-profiling technologies for academic drug discovery.

Drug discovery within Academia is now firmly established and typically uses technologies that are based on historical Pharmaceutical industry paradigms. New technologies, now being adopted by the Pharmaceutical industry, offer advantages over traditional screening and compound-profiling techniques. These approaches mark a departure from the ‘one gene, one protein, one target, one compound’ model. This review covers the benefits which are achievable if academic drug discovery organisations were to look beyond microplate-based screening.

[1]  T. Clackson,et al.  Translational Research in Academia and Industry , 2006, Experimental biology and medicine.

[2]  Herbert Waldmann,et al.  Chemical biology--identification of small molecule modulators of cellular activity by natural product inspired synthesis. , 2008, Chemical Society reviews.

[3]  Phillip Gribbon,et al.  High-throughput drug discovery: what can we expect from HTS? , 2005, Drug discovery today.

[4]  N. Blow Lab automation: tales along the road to automation , 2008, Nature Methods.

[5]  Joe D. Lewis,et al.  The structural basis for cap binding by influenza virus polymerase subunit PB2 , 2008, Nature Structural &Molecular Biology.

[6]  K. Hofbauer Academic institutions and industry: bridging the gap , 2008, Expert opinion on drug discovery.

[7]  S. Ley,et al.  Pharmaceutical Strategy and Innovation: An Academics Perspective , 2007, ChemMedChem.

[8]  Benjamin F. Cravatt,et al.  Genomics and proteomics: From genes to function: advances in applications of chemical and systems biology , 2007 .

[9]  Dan C. Fara,et al.  Lead-like, drug-like or “Pub-like”: how different are they? , 2007, J. Comput. Aided Mol. Des..

[10]  David R Spring,et al.  Chemical genetics to chemical genomics: small molecules offer big insights. , 2005, Chemical Society reviews.

[11]  E. Krausz,et al.  High-content siRNA screening. , 2007, Molecular bioSystems.

[12]  György Kéri,et al.  Cellular targets of gefitinib. , 2005, Cancer research.

[13]  Christopher P Austin,et al.  High-throughput screening assays for the identification of chemical probes. , 2007, Nature chemical biology.

[14]  T. Spicer,et al.  Comparison of Miniaturized Time-Resolved Fluorescence Resonance Energy Transfer and Enzyme-Coupled Luciferase High-Throughput Screening Assays to Discover Inhibitors of Rho-Kinase II (ROCK-II) , 2008, Journal of biomolecular screening.

[15]  Anang A Shelat,et al.  The interdependence between screening methods and screening libraries. , 2007, Current opinion in chemical biology.

[16]  H. Daub Characterisation of kinase-selective inhibitors by chemical proteomics. , 2005, Biochimica et biophysica acta.

[17]  Alexander Tropsha,et al.  Why Academic Drug Discovery Makes Sense , 2006, Science.

[18]  Timothy J Mitchison,et al.  Small‐Molecule Screening and Profiling by Using Automated Microscopy , 2005, Chembiochem : a European journal of chemical biology.

[19]  Samu Melkko,et al.  DNA-encoded chemical libraries , 2022, Nature Reviews Methods Primers.

[20]  Christoph E. Dumelin,et al.  Lead discovery by DNA-encoded chemical libraries. , 2007, Drug discovery today.

[21]  John S Lazo,et al.  Building a Pharmacological Lexicon: Small Molecule Discovery in Academia , 2007, Molecular Pharmacology.

[22]  R. Lerner,et al.  Encoded combinatorial chemistry. , 1992, Proceedings of the National Academy of Sciences of the United States of America.

[23]  Herbert Waldmann,et al.  Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis. , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[24]  Michael Snowden,et al.  The impact of diversity-based, high-throughput screening on drug discovery: "chance favours the prepared mind". , 2008, Current opinion in drug discovery & development.

[25]  Timothy J Mitchison,et al.  Small molecule screening by imaging. , 2006, Current opinion in chemical biology.

[26]  Xiaobo Zhou,et al.  Informatics challenges of high-throughput microscopy , 2006, IEEE Signal Processing Magazine.

[27]  G. Drewes,et al.  Chemical and Pathway Proteomics , 2008, Molecular & Cellular Proteomics.

[28]  Wei Zhang,et al.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2007. , 2008, Journal of combinatorial chemistry.

[29]  A. Verkman Drug discovery in academia. , 2004, American journal of physiology. Cell physiology.

[30]  Ricardo Macarron,et al.  Critical review of the role of HTS in drug discovery. , 2006, Drug discovery today.

[31]  Alastair Binnie,et al.  Case study: impact of technology investment on lead discovery at Bristol-Myers Squibb, 1998-2006. , 2008, Drug discovery today.

[32]  Sam Michael,et al.  A robotic platform for quantitative high-throughput screening. , 2008, Assay and drug development technologies.

[33]  K. Yeow,et al.  Cellular imaging in drug discovery , 2006, Nature Reviews Drug Discovery.

[34]  R. Pepperkok,et al.  The potential of high‐content high‐throughput microscopy in drug discovery , 2007, British journal of pharmacology.

[35]  Andreas Sewing,et al.  Helping science to succeed: improving processes in R&D. , 2008, Drug discovery today.

[36]  Eric D. Brown,et al.  High-Throughput Screening at McMaster University: Automation in Academe , 2004 .

[37]  C. Tralau-Stewart,et al.  Drug discovery: new models for industry-academic partnerships. , 2009, Drug discovery today.