Probing Cancer with Small-molecule Tools-Progress and Challenges

Chemical probes are powerful small-molecule tools in fundamental and translational cancer research. They are highly versatile, complementing genetic technologies in the annotation of protein function, and invaluable in target validation and drug discovery. However, continued improvements are needed to enhance best practices in selection and use of chemical probes. We discuss progress over the last decade, highlight key issues, and indicate a path to generate a high-quality chemical probe for every human protein.