The microarrays will be used for characterisation of lead compounds, including selectivity, potency (IC50) and mechanism of action studies for signal transduction-focused medicinal chemistry groups.
The joint technology has been developed through close co-operation from the pharmaceutical industry and scientific advisors. Dr Rob Ruijtenbeek, head of kinase research at PamGene said that this technology will reduce the cost of the drug discovery process.
"One of the main challenges in pharma R&D is improving compound selection. With PamGene's 96-well array platform and JPT's kinase peptide substrates, it is now possible to generate kinetic read-out of multiple kinase activities in one experiment."
"Additionally, we can analyse multiple conditions on a single plate, e.g. inhibitor concentration series. The content and kinetic data will allow intelligent selection and prioritisation of leads that enter the subsequent stages of drug development."
JPT's technology enables parallel syntheses and screening of peptide leads, pharmacophore identification and transformation into pepti-domimetic and small molecule drugs.
The peptide lead to small molecule conversion process is supported by medicinal chemistry and cheminformatics and guided by matching the pharmacophore derived from massive peptide SAR data information against a virtual small molecule library. Jerini's platform allows the rapid identification and/or optimisation of agonists and antagonists for difficult target proteins.