(-)-FR182877 Is a Potent and Selective Inhibitor of Carboxylesterase-1

Gregory C. Adam, Christopher D. Vanderwal, Erik J. Sorensen, Benjamin F. Cravatt

Research output: Contribution to journalArticle

48 Scopus citations

Abstract

Activity-based profiling and reporter-group-tagged compounds were used to identify carboxylesterase-1 (CE-1) as a specific target of the natural product (-)-FR182877 (see scheme). Now that a target is known, specific modification of the lactone natural product may lead to even more effective inhibitors of CE-1.

Original languageEnglish (US)
Pages (from-to)5480-5484
Number of pages5
JournalAngewandte Chemie - International Edition
Volume42
Issue number44
DOIs
StatePublished - Nov 17 2003

All Science Journal Classification (ASJC) codes

  • Catalysis
  • Chemistry(all)

Keywords

  • Activity-based profiling
  • Hydrolases
  • Inhibitors
  • Natural products
  • Proteomics

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