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

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 p...

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Bibliographic Details
Published in:Chembiochem : a European journal of chemical biology 2005-02, Vol.6 (2), p.287-291
Main Authors: Borodovsky, Anna, Ovaa, Huib, Meester, Wim J.N, Venanzi, Emily S, Bogyo, Matthew S, Hekking, Brian G, Ploegh, Hidde L, Kessler, Benedikt M, Overkleeft, Herman S
Format: Article
Language:English
Subjects:
active-site-directed probe
Amino Acid Sequence
Endopeptidases - chemistry
Endopeptidases - genetics
Endopeptidases - metabolism
enzymes
Molecular Structure
Peptides - chemistry
Peptides - genetics
Peptides - metabolism
Protease Inhibitors - metabolism
proteases
protein modifications
Protein Processing, Post-Translational
Sulfones - chemistry
SUMO APG
SUMO-1 Protein - genetics
SUMO-1 Protein - metabolism
ubiquitin
Ubiquitin - chemistry
Ubiquitin - genetics
Ubiquitin - metabolism
Ubiquitin-Specific Proteases
Vinyl Compounds - chemistry
vinyl sulfones
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Summary: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.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.200400236