Small-molecule inhibitors and probes for ubiquitin- and ubiquitin-like-specific proteases

Anna Borodovsky, Huib Ovaa, Wim J.N. Meester, Emily S. Venanzi, Matthew S. Bogyo, Brian G. Hekking, Hidde L. Ploegh, Benedikt M. Kessler, Herman S. Overkleeft

Research output: Contribution to journalArticlepeer-review

72 Scopus citations

Abstract

There's always a catch. The post-translational modification of proteins with ubiquitin (Ub) or ubiquitin-like (Ubl) modifiers is an important signal in the regulation of a variety of biological processes, such as degradation and regulation of gene expression. Here we report the synthesis of a panel of peptide vinyl sulfones (see scheme) harboring various portions of the Ub C terminus by using a safety-catch linker. Depending on their length, such compounds can efficiently target Ubl-specific proteases.

Original languageEnglish
Pages (from-to)287-291
Number of pages5
JournalChemBioChem
Volume6
Issue number2
DOIs
StatePublished - Feb 2005
Externally publishedYes

Keywords

  • Active-site-directed probe
  • Enzymes
  • Proteases
  • Protein modifications
  • SUMO APG
  • Ubiquitin
  • Vinyl sulfones

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