There are over 500 protein kinases in the human kinome. These enzymes are responsible for cell signalling mechanisms that control a wide spectrum of physiological processes. Consequently, the regulation/ misregulation of kinases has linked them to a number of diseases and they provide a wealth of opportunity as targets for drug discovery. To highlight these opportunities, Protein Kinase 2009: signalling success took place at AstraZeneca, Cheshire, UK on 18-19 May 2009. The symposium showcased some of the current research into this family of enzymes.
Plenary lectures were given by David Rees (Astex Therapeutics), Stefan Knapp (Structural Genomics Consortium) and Richard Morphy (Schering-Plough). These presentations will give an overview of the structure and function of kinases. They described different approaches and issues associated with the identification and optimisation of inhibitors of this class of enzymes. In a keynote lecture, Professor Malcolm Ranson (University of Manchester / Christie Hospital) provided an insight into the clinical aspects of developing kinase inhibitors as effective medicines.
To date, all of the kinase inhibitor drugs on the market are for use in an oncology setting. Bernd Riedl (Bayer HealthCare AG) will describe the discovery of one of these marketed drugs, Sorafenib/ Nexavar, which is prescribed for kidney and liver cancers. Several other talks focused on some of the possible next-generation small molecule chemotherapies for cancer treatment. Vertex described its progress on inhibition of Flt-3, AstraZeneca presented on mTor inhibitors and Boehringer Ingelheim discussed its programme on Plk1 inhibitors.
Additional presentations detailed kinase inhibitors, which have potential for the treatment of diseases in therapeutic areas other than cancer. These included a talk on GSK3 inhibitors for Alzheimer’s disease and JNK inhibitors for type II diabetes. The symposium will conclude with a round table discussion, providing delegates with the opportunity to field questions to a panel of experts.
Dr Stephen East, SCI Fine Chemicals Technical Group and Evotec (UK) Ltd