Protein-reactive natural products

Carmen Drahl, Benjamin F. Cravatt, Erik J. Sorensen

Research output: Contribution to journalReview articlepeer-review

213 Scopus citations


Researchers in the post-genome era are confronted with the daunting task of assigning structure and function to tens of thousands of encoded proteins. To realize this goal, new technologies are emerging for the analysis of protein function on a global scale, such as activity-based protein profiling (ABPP), which aims to develop active site-directed chemical probes for enzyme analysis in whole proteomes. For the pursuit of such chemical proteomic technologies, it is helpful to derive inspiration from protein-reactive natural products. Natural products use a remarkably diverse set of mechanisms to covalently modify enzymes from distinct mechanistic classes, thus providing a wellspring of chemical concepts that can be exploited for the design of active-site-directed proteomic probes. Herein, we highlight several examples of protein-reactive natural products and illustrate how their mechanisms of action have influenced and continue to shape the progression of chemical proteomic technologies like ABPP.

Original languageEnglish (US)
Pages (from-to)5788-5809
Number of pages22
JournalAngewandte Chemie - International Edition
Issue number36
StatePublished - Sep 4 2005

All Science Journal Classification (ASJC) codes

  • General Chemistry
  • Catalysis


  • Enzymes
  • Inhibitors
  • Molecular probes
  • Natural products
  • Structure-activity relationships


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