Small molecule drug discovery has approached a critical junction where the rigorous pre-clinical validation and prioritizing of novel targets is of utmost importance. Challenged with thinning development pipelines and significant losses in revenue, greater emphasis is being placed on the stringent selection and validation of targets and candidate molecules to increase success and reduce attrition rates in phase II trials. In response to this challenge, a synergy between drug discovery and chemical biology is emerging as a vital component to providing adequate confidence before launching full discovery programs. The development and utilization of high-quality chemical probes in combination with disease-relevant phenotypic systems provides a powerful approach to obtain a deeper interrogation of target-phenotype relationships - ultimately enriching target validation.
Selecting and Modulating Therapeutic Targets Using Human Biology and Chemical Biology
Stuart L. Schreiber, Ph.D., Director, Center for the Science of Therapeutics & Founding Member, Broad Institute of Harvard and MIT; Howard Hughes Medical Institute Investigator; Morris Loeb Professor, Chemistry and Chemical Biology, Harvard University
Structures, Chemical Probes, New Biology, New Targets for Drug Discovery: Is This the Right Sequence?
Chas Bountra, Ph.D., Professor, Translational Medicine; Head, Structural Genomics Consortium, University of Oxford
Covalent Inhibitors of Oncogenic Signaling Pathways
Nathanael Gray, Ph.D., Professor, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School; Professor, Cancer Biology, Dana-Farber Cancer Institute
Genome-Wide Spatial Localization of Small Molecules
James E. Bradner, M.D., Assistant Professor, Department of Medicine, Harvard Medical School and Investigator, Department of Medical Oncology, Dana-Farber Cancer Institute