Small‐Molecule Inhibitors and Probes for Ubiquitin‐ and Ubiquitin‐Like‐Specific Proteases

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

ChemBioChem · 2005 · 77 citations · 32 references

Concepts

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.

References

32