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Glycine fluoromethylketones as SENP-specific activity based probes.
Dobrota, Cristian; Fasci, Domenico; Hadade, Niculina D; Roiban, Gheorghe-Doru; Pop, Cristina; Meier, Veronika M; Dumitru, Ioana; Matache, Mihaela; Salvesen, Guy S; Funeriu, Daniel P.
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  • Dobrota C; Department of Chemistry, Technical University of Munich, Garching, Germany.
Chembiochem ; 13(1): 80-4, 2012 Jan 02.
Article en En | MEDLINE | ID: mdl-22134988
We report here the synthesis and biochemical properties of a new peptidyl activity-based probe 1 for SUMO proteases, SENPs. The activity-based probe has at its C terminus a glycine-derived fluoromethylketone moiety as a reactive group designed to target the active-site cysteine of SENPs. Based on a study of the interactions between SENPs and SUMOs, we introduced further design elements that allow the activity-based probe to selectively target SENPs at low micromolar to high nanomolar concentrations. Moreover, 1 out-competes SUMO1 from the reversible SUMO1-SENP1 complex, thus suggesting that 1 and SUMO1 share a common binding site on SENP1.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Endopeptidasas / Colorantes Fluorescentes / Glicina / Cetonas Límite: Humans Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2012 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Alemania
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Endopeptidasas / Colorantes Fluorescentes / Glicina / Cetonas Límite: Humans Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2012 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Alemania