Bio-organic chemistry and Chemical biology

After the elucidation of the genomes of several organisms the field of proteomics now faces the task to identify and characterize the functions of the genome products (i.e. the expressed proteins in a cell, tissue or organism). Most proteomic experiments deal with global monitoring of protein abundance, which is not necessarily related to function and activity. In particular, enzymes are tightly regulated through post-translational processes. Thus, to uncover the functions of enzymes during physiological and pathological processes, it is desirable to specifically monitor the dynamic levels of their activities.
   Chemical or activity-based proteomics uses small molecule probes to specifically modify small subsets of active enzymes. This allows to focus on particular proteins that are responsible for crucial biochemical transformations.
   The small molecules used in chemical proteomics are termed activity-based probes (ABPs) and consist of three basic elements (see Figure 1): a reactive warhead that is able to covelently modify an enzyme’s active site, a tag that facilitates enrichment and/or visualization of the enzyme activity, and a spacer that both separates the two previous elements and influences the selectivity of the reactive warhead.

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