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Content archived on 2024-06-16

Protein kinases - Novel Drug Targets of Post Genomic Era


Nearly all aspects of cell life (and death) are controlled by protein phosphorylation catalysed by protein kinases (PKs). PKs belong to the largest single family of enzymes, numbering over 500 and accouting for almost 2% of the proteins encoded by the human genome. Recent success in drug discovery (e.g. Imatinib, GlivecR) demonstrate that PKs are excellent drug targets. The Pro-KinaseResearch consortium will combine European expertise on basic research on PKs and that on rational drug discovery, in order to develop new drug candidates and treatment strategies for major diseases like cancer, autoimmune disorders, vascular diseases and degenerative brain diseases. Thus, the aim of this IP is to study PKs as drug targets for more effective and better tolerated drug therapies meeting the needs of ageing population.

The joint effort will focus on the biochemical properties and structure function relationships of a wide variety of PKs having the potential as pharmacological targets. We will evaluate the regulatory domains, catalytic domains and also anchoring proteins of various PKs, as drug targets. Natural compounds from European biosphere, e.g. Cyanobacteria, and compounds from combinatorial chemistry, chemical libraries, affecting activity of PKs will be analysed to gain knowledge of their structure/activity relationship. These compounds will be used as model drugs or templates for a rational drug design where new compounds will be modelled and synthesised. This consortium has a broad range of bioactivity assays to study the efficacy and toxicity of the new compounds. The consortium includes academic groups with unique expertise in biochemistry, structural crystallography, synthetic organic chemistry, lead structure optimisation and other fields of rational drug discovery; clinically oriented groups with proven experience in animal models and phase I-II clinical studies under GCP guidelines; and SME partners to assure a quick transfer of knowledge.

Call for proposal

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Participants (27)