Cancer Institute A national cancer institute
designated cancer center

Matthew Bogyo

Publication Details

  • Development of Small Molecule Inhibitors and Probes of Human SUMO Deconjugating Proteases CHEMISTRY & BIOLOGY Albrow, V. E., Ponder, E. L., Fasci, D., Bekes, M., Deu, E., Salvesen, G. S., Bogyo, M. 2011; 18 (6): 722-732


    Sentrin specific proteases (SENPs) are responsible for activating and deconjugating SUMO (Small Ubiquitin like MOdifier) from target proteins. It remains difficult to study this posttranslational modification due to the lack of reagents that can be used to block the removal of SUMO from substrates. Here, we describe the identification of small molecule SENP inhibitors and active site probes containing aza-epoxide and acyloxymethyl ketone (AOMK) reactive groups. Both classes of compounds are effective inhibitors of hSENPs 1, 2, 5, and 7 while only the AOMKs efficiently inhibit hSENP6. Unlike previous reported peptide vinyl sulfones, these compounds covalently labeled the active site cysteine of multiple recombinantly expressed SENP proteases and the AOMK probe showed selective labeling of these SENPs when added to complex protein mixtures. The AOMK compound therefore represents promising new reagents to study the process of SUMO deconjugation.

    View details for DOI 10.1016/j.chembiol.2011.05.008

    View details for Web of Science ID 000292583800007

    View details for PubMedID 21700208

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