A fundamental challenge to the future of oncology drug discovery is the identification of the next generation of well-validated molecular targets. Kinase targets in particular have received considerable attention over the last decade due to their ability to be effectively inhibited by small molecule or biologic agents and to provide therapeutic benefit for cancer patients. However, much less attention has been focused on the advancement of non-kinase molecular targets for oncology drug discovery due to concerns related to the ability of such targets to be modulated by small molecules, development of robust screening assays and selectivity against related proteins. This session will highlight the discovery of small molecule inhibitors for three novel molecular targets that represent emerging areas for therapeutic intervention in cancer and provide a forum to review the challenges associated with the advancement of such targeting opportunities.
Educational Session: From Chemistry to the Clinic: Pathways for Drug Discovery and Development: Part 2: Emerging Molecular Targets

Introduction; Matthew V. Lorenzi. Bristol-Myers Squibb Company, Princeton, NJ

Discovery of small molecule sirtuin inhibitors through a p53 activation assay; Sonia Lain. University of Dundee, Dundee, United Kingdom

Selectively targeting protein ubiquitination with an inhibitor of Nedd8 activating enzyme; Teresa Soucy. Millennium Pharmaceuticals, Cambridge, MA

Targeting notch in cancer with gamma secretase inhibitors; Christopher G. Winter. Merck Research Laboratories, Boston, MA,