Targeting Kinases for Drug Discovery

Protein kinases - intracellular enzymes that modulate cellular functions - play a pivotal role in the signal transduction processes that regulate many key biological processes. Abnormalities in these signal transduction pathways are implicated in the etiology of numerous diseases, which has motivated pharmaceutical companies to pursue protein kinases as drug targets - a trend that now accounts for 20-30% of all drug discovery programs.

• The protein kinase family is a mostly unexploited class of drug targets. Novartis' s kinase inhibitor Gleevec, approved in 2001 for CMS, boasts sales of $3 billion worldwide in 2007. What effect has Gleevec' s success had on the development of new kinase inhibitors?
• Most major pharmaceutical companies are avidly pursuing kinase inhibitor development both internally and/or in collaboration with biotech companies. Which Big Pharma players have kinase inhibitor development programs underway? What are some of the key collaborations and alliances that have formed around kinase targets? What is the current state of the kinase inhibitor development pipeline?
• Whereas development of kinase inhibitors in the past has been hindered by the perceived complexity of the process, technological advances will drive the future development of kinase inhibitors. What are some of the technologies that have aided the development of new kinase inhibitors? How has technology altered the choice of drug targets and disease indications being pursued by pharma companies?
• At present, oncology patients have derived the most benefit from kinase inhibitors, although the potential exists for patients with longer-term chronic conditions to benefit. What chronic conditions are under investigation for treatment with kinase inhibitors? What difficulties or opportunities lie on the path of such agents' approval?

• Commercial potential: current state of the kinase inhibitor market; potential market influences.
• About protein kinases: protein kinase family classifications; structure and function of the kinase and its inhibitors; current screening procedures.
• Kinase inhibitor selectivity: why selectivity is important and how it can be determined.
• Development challenges: the influences of mutations and drug resistance; p38 MAP kinases.
• Pharmacogenomics: the influence of genetic variation on kinase inhibitor efficacy.
• Profiles: select companies employing novel technologies and strategies in kinase research.
• Market outlook: our general forecast for the direction and success of protein kinase inhibitors.