Drug Targets – Multimedia

Pseudomonas elastase (LasB) is a key drug target in various chronic and intractable infections. A library of 160 potential, in-house synthesised, elastase inhibitors were screened using a fluorescence assay with the internally quenched substrate Abz-Ala-Gly-Leu-Ala-Nba. Enzymatic kinetic measurements were done on a FLUOstar OPTIMA and Km and Vmax values were calculated for each inhibitor using the MARS Data Analysis software.

Thousands of formalin-fixed, paraffin-embedded (FFPE) samples from clinical archives are available for retrospective studies. Such samples could provide crucial information for drug target discovery and diagnostics of various diseases. Here we used FFPE samples and their matched fresh-frozen (FF) counterparts to examine their performance on three types of microarrays including whole genome expression, comparative genomic hybridization (CGH) and microRNA.

Thousands of formalin-fixed, paraffin-embedded (FFPE) samples from clinical archives are available for retrospective studies. Such samples could provide crucial information for drug target discovery and diagnostics of various diseases. Here we used FFPE samples and their matched fresh-frozen (FF) counterparts to examine their performance on three types of microarrays including whole genome expression, comparative genomic hybridization (CGH) and microRNA.

Tyrosine kinases are important regulators in cellular processes. Kinases have been found to be involved in diseases such as cancer and cardiovascular, therefore, molecules that modulate kinase function are expected to be promising new drug targets. In this poster, we will describe the performance of an AlphaScreen™ (amplified luminescent proximity homogeneous assay) tyrosine kinase assay on BMG LABTECH´s PHERAstar using an AlphaScreen™ specific excitation LASER.

To facilitate the rapid identification of PDE inhibitors, BellBrook Labs has developed a fluorescence polarization immunoassay that directly detects AMP and GMP. The Transcreener™ PDE Assay includes a single set of reagents - an anti-AMP/GMP antibody and fluorescent tracer - that can be used for any cyclic nucleotide PDE, providing a robust, cost-effective alternative to currently available technologies.

To facilitate the rapid identification of PDE inhibitors, BellBrook Labs has developed a fluorescence polarization immunoassay that directly detects AMP and GMP. The Transcreener™ PDE Assay includes a single set of reagents - an anti-AMP/GMP antibody and fluorescent tracer - that can be used for any cyclic nucleotide PDE, providing a robust, cost-effective alternative to currently available technologies.

Three pharmacophore searching methods were applied to finding potential ATP-competitive inhibitors of the Tyrosine Kinase family: i) manual pharmacophore modeling (MOE), ii) “fuzzy” pharmacophore models (SQUID), and iii) similarity searching based on correlation-vector representations of potential pharmacophore-points (CATS3D).

The activation of GPCRs is known to lead to the dynamic translocation of multiple signaling molecules or molecular assemblies during its signaling cycle, and in many cases cytoskelatal reorganization. Such a movement and/or reorganization results in dynamic redistribution of cellular contents, equivalent to dynamic mass redistribution (DMR), which can be monitored online in living cells using Corning® Epic™ system – a label-free and non-invasive biosensor system.