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Activity-based probes for monitoring postproline protease activity

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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.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.issn 1439-4227
dc.identifier.uri http://hdl.handle.net/10230/37081
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.language.iso eng
dc.publisher Wiley-VCH Verlag
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.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.identifier.doi http://dx.doi.org/10.1002/cbic.200900244
dc.rights.accessRights info:eu-repo/semantics/openAccess
dc.type.version info:eu-repo/semantics/acceptedVersion

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