Small-Molecule Inhibitors and Probes for Ubiquitin- and Ubiquitin-Like-Specific Proteases (pages 287–291)
Anna Borodovsky, Huib Ovaa, Wim J. N. Meester, Emily S. Venanzi, Matthew S. Bogyo, Brian G. Hekking, Hidde L. Ploegh, Benedikt M. Kessler and Herman S. Overkleeft
Article first published online: 13 JAN 2005 | DOI: 10.1002/cbic.200400236
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.