EC-FP6-LIFESCIHEALTH: Protein kinases - Novel Drug Targets of Post Genomic Era (PRO-KINASE RESEARCH), LSH-2002-1.2.1-1 Screening for drug candidates targeting aberrant molecular signalling in protein phosphorylation pathways (Integrated Project)



The project objective is to develop protein kinase inhibitors and activators based on a combination of design and screening by using natural compounds from the European biosphere in addition to chemical libraries. Protein kinases (PKs) belong to the largest single family of enzymes, numbering over 500 and accounting for almost 2% of the proteins encoded by the human genome. Recent success in drug discovery demonstrates that PKs are excellent drug targets.

The Pro-Kinase Research consortium combines 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 Consortium partners have already during this project prepared several hundred natural extracts, pure compound isolations and synthetic compounds. The bioactivity of many of these compounds has been tested. Several promising lead compounds have been found for further development of drugs for treating atherosclerosis, leukemia, parasite diseases or neuroprotective agents in stroke and epilepsy. The Consortium is also actively developing new methods and improving old ones for the characterisation and testing the potential PK-targeted compounds. The bioactivity assays need large quantities of PK proteins and some Consortium partners are producing these proteins for assay purposes. Also, some laboratories are producing PK proteins in order to determine their three-dimensional structure for the rational drug design.

The Consortium aims at the discovery of new means by which the activity of PKs can be modified, and therefore making way to development of clinically useful drugs having a novel mechanism of action. These new drugs will help both the developed (cancer, cardiovascular diseases) and developing countries (parasitic infectious diseases).
Gällande start-/slutdatum01/03/200431/08/2009