Focus on Chemical Probes

Chemical biologists are making significant progress in discovering and characterizing high-quality chemical probes. In this issue, we feature Commentary and Review Articles that capture opinions and advances at the frontiers of chemical probe research.



Focus on Chemical Probes

Retooling chemical probes p157


Increased transparency and consistency in reporting well-validated chemical probes will further enhance the impact of this exciting and rapidly advancing area of chemical biology.



Focus on Chemical Probes

The art of the chemical probe pp159 - 161

Stephen V Frye


Chemical biologists frequently aim to create small-molecule probes that interact with a specific protein in vitro in order to explore the role of the protein in a broader biological context (cells or organisms), but a common understanding of what makes a high-quality probe is lacking. Here I propose a set of principles to guide probe qualification.

Focus on Chemical Probes

Rethinking screening pp162 - 165

Thomas Kodadek


Bioactive compounds are most frequently identified via high-throughput screening campaigns. This article discusses the strengths and weaknesses of the most popular screening approaches and the utility of compounds derived from them.

Focus on Chemical Probes

The (un)targeted cancer kinome pp166 - 169

Oleg Fedorov, Susanne Müller & Stefan Knapp


The complexity of cancer signaling and the resulting difficulties in target selection have strongly biased kinase drug discovery towards clinically validated targets. Recently, novel kinase targets that are uncharacterized have emerged from genome sequencing and RNAi studies. Chemical probes are urgently needed to functionally annotate these kinases and to stimulate new drug discovery efforts.



Focus on Chemical Probes

Turning enzymes ON with small molecules pp179 - 188

Julie A Zorn & James A Wells


Focus on Chemical Probes

Garbled messages and corrupted translations pp189 - 198

Tilman Schneider-Poetsch, Takeo Usui, Daisuke Kaida & Minoru Yoshida


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