Activity-based probes for monitoring postproline protease activity

Mostra el registre complet Registre parcial de l'ítem

• dc.contributor.author Sabidó Aguadé, Eduard, 1981-
• dc.contributor.author Tarragó, Teresa
• dc.contributor.author Niessen, Sherry
• dc.contributor.author Cravatt, Benjamin F.
• dc.contributor.author Giralt, Ernest
• dc.date.accessioned 2019-04-10T08:37:04Z
• dc.date.available 2019-04-10T08:37:04Z
• dc.date.issued 2009
• dc.description.abstract Postproline proteases constitute a subset of serine proteases involved in the regulation of many signaling events and are emerging as promising therapeutic targets for prevalent diseases, such as diabetes and cancer. Therefore, monitoring their activity in different tissues and diverse physiological states would certainly facilitate the elucidation of their physiological role and the establishment of new therapeutic targets. Here, we have synthesized a dipeptidyl phosphonate activity-based probe that has proved to be highly selective for a specific postproline protease, prolyl oligopeptidase (POP). Its high sensitivity allows the detection of the endogenous activity of POP both by in-gel analysis and mass spectrometry. The evidence provided by mass spectrometry for the high selectivity of the synthesized probe opens the possibility of using dipeptidyl phosphonates not only for activity-based profiling (ABP), but also for other ABP applications like substrate-based protease identification.
• dc.description.sponsorship This work was supported by MCYT-FEDER (Bio2005–00 295 and NAN2004-09 159-C04–02) and Generalitat de Catalunya (CERBA and 2005SGR-00 663). E.S. was supported by a grant from Ministerio de Educación y Ciencia, Spain
• dc.format.mimetype application/pdf
• dc.identifier.citation Sabidó E, Tarragó T, Niessen S, Cravatt BF, Giralt E. Activity-based probes for monitoring postproline protease activity. Chembiochem. 2009 Sep 21;10(14):2361-6. DOI: 10.1002/cbic.200900244
• dc.identifier.doi http://dx.doi.org/10.1002/cbic.200900244
• dc.identifier.issn 1439-4227
• dc.identifier.uri http://hdl.handle.net/10230/37081
• dc.language.iso eng
• dc.publisher Wiley-VCH Verlag
• dc.relation.ispartof Chembiochem. 2009 Sep 21;10(14):2361-6
• dc.rights © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. Activity-based probes for monitoring postproline protease activity. Eduard Sabidó et al. Chembiochem, vol. 10, núm. 14
• dc.rights.accessRights info:eu-repo/semantics/openAccess
• dc.subject.other Compostos organofosforats
• dc.subject.other Proteases serines
• dc.title Activity-based probes for monitoring postproline protease activity
• dc.type info:eu-repo/semantics/article
• dc.type.version info:eu-repo/semantics/acceptedVersion