Chemical Probe Synthesis and Applications in Chemical Biology

Dear Colleagues,

A chemical probe can be considered a cell permeable small-molecule modulator, typically an inhibitor, with defined selectivity and affinity for a specific biological macromolecule, most commonly a protein. Chemical probes with high affinity and selectivity allow the study of phenotypes associated with a specific protein. Such probes can be aids in drug target validation and complementary tools to genetic approaches. The perception of chemical probes, as mainly small-molecule inhibitors, could perhaps broaden with an increase in prevalence of selective protein–protein interaction modulators, heterobifunctional protein degraders, and cell permeable and stapled peptides. Chemical probes can be further functionalised with fluorophores, photoreactive groups, biotin, or bio-orthogonal functional groups for in cell labelling. This facilitates not only the study of phenotypes associated with the protein, but also in-cell imaging, quantifying enzymatic activity, and identifying other potential protein binding partners via protein–protein complexes and potential ‘off-target’ protein interactions. Despite these advances, not one approach to the development of chemical probes is amenable for all proteins or biological macromolecules. High affinity, selectivity, and cell permeability still remain significant hurdles to the development of high quality chemical probes. This is an exciting and rapidly developing field of research to which synthetic chemists and chemical biologists can contribute through the design and synthesis of new chemical probes. We invite original research articles or review contributions to this Special Issue on chemical probes, in all aspects of chemical probes including design, synthesis, optimisation studies, methodologies of use, and applications in all areas of chemical biology.

Dr. James T. Hodgkinson
Guest Editor

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