Protein kinases are the workhorses of cellular regulation, playing a key role in almost every major pathway in eukaryotic cells, including those that control cell division, cell death, cell growth, and programs of differentiation. These proteins play key regulatory roles in plants and bacteria, including many pathogenic microorganisms. Mutations or overexpression of these proteins is implicated in a wide range of diseases, from cancer to diabetes to neurodegenerative diseases.
An April 28, 2009, meeting of the Academy's Chemical Biology Discussion Group featured four researchers who study kinase structure and function and are working to develop these findings into effective therapeutics. Topics discussed included newly identified, potentially druggable targets in protein kinase A; challenges to kinase-directed drug development, including problems related to toxicity, selectivity, efficacy, and patentability; and advances in the relatively new field of fragment-based drug design, in which small chemical fragments are identified by screening as starting points to build larger, drug-like compounds with favorable physicochemical and clinical properties.
In this Webinar
Video
Protein Kinases: Dynamic Targets for Drug Design
Susan Taylor (University of California, San Diego)
Slides & Audio
Structure-based Drug Design on Kinase Targets: Key Lessons Learned
Vincent Stoll (Abbott Laboratories)
Slides & Audio
Fragment-based Drug Discovery
Harren Jhoti (Astex Therapeutics)
Slides & Audio
Structure/Fragment Based Drug Discovery for Protein Kinases
Stephen Burley (Eli Lilly and Co.)