Screening Europe 2010: an update about the latest technologies and applications in high-throughput screening

This article reviews important presentations from the 7th Screening Europe Conference, and extracts general trends and developments. Technological advances, as well as novel applications are discussed, thus providing an overview on state-of-the-art high-throughput screening. Among other topics, cell-based assays were highly popular, since they reflect the clinical situation much more closely than screens based on purified drug targets. A further approach to reduce the costly attrition of drug candidates subsequent to initial screens is the use of label-free technology. By measuring desired properties directly, without the use of any reporter (e.g., calorimetric measurements of binding affinities), the selection of false positives can be decreased drastically. Additional improvements in high-throughput screening are resulting from novel technology platforms utilizing sophisticated imaging systems and/or miniaturization. These and other important topics from the Screening Europe 2010 Conference are discussed in this article, thus providing a current snapshot of the field.

[1]  D. Connolly,et al.  (d)-β-Hydroxybutyrate Inhibits Adipocyte Lipolysis via the Nicotinic Acid Receptor PUMA-G* , 2005, Journal of Biological Chemistry.

[2]  M. Klein,et al.  A Unitary Anesthetic Binding Site at High Resolution* , 2009, The Journal of Biological Chemistry.

[3]  Tudor I. Oprea,et al.  The Design of Leadlike Combinatorial Libraries. , 1999, Angewandte Chemie.

[4]  Christoph A. Merten,et al.  High-throughput screening of enzymes by retroviral display using droplet-based microfluidics. , 2010, Chemistry & biology.

[5]  John A. Tallarico,et al.  Multi-parameter phenotypic profiling: using cellular effects to characterize small-molecule compounds , 2009, Nature Reviews Drug Discovery.

[6]  Christoph A. Merten,et al.  Droplet-based microfluidic platforms for the encapsulation and screening of Mammalian cells and multicellular organisms. , 2008, Chemistry & biology.

[7]  Andrew D Griffiths,et al.  An automated two-phase microfluidic system for kinetic analyses and the screening of compound libraries. , 2010, Lab on a chip.

[8]  Christoph A. Merten,et al.  A competition-based assay for the screening of species-specific antibiotics. , 2009, The Journal of antimicrobial chemotherapy.

[9]  P. Graczyk Gini coefficient: a new way to express selectivity of kinase inhibitors against a family of kinases. , 2007, Journal of medicinal chemistry.

[10]  R. Eglen,et al.  An overview of drug screening using primary and embryonic stem cells. , 2008, Combinatorial chemistry & high throughput screening.

[11]  Mindy I. Davis,et al.  A quantitative analysis of kinase inhibitor selectivity , 2008, Nature Biotechnology.

[12]  N. Socci,et al.  High-throughput screening assay for the identification of compounds regulating self-renewal and differentiation in human embryonic stem cells. , 2008, Cell stem cell.

[13]  J. Violin,et al.  beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice. , 2009, The Journal of clinical investigation.