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Conjugation of a Novel Apaf-1 Inhibitor to Peptide-based Cell-Membrane Transporters. Effective Methods to Improve Inhibition of Mitochondria-Mediated Apoptosis

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dc.creator Orzáez, Mar
dc.creator Mondragón Martínez, Laura
dc.creator Marzo, Isabel
dc.creator Sanclimens Pérez de Rozas, Gloria
dc.creator Messeguer Peypoch, Ángel
dc.creator Pérez-Payá, Enrique
dc.creator Vicent, María J.
dc.date 2008-05-19T09:30:58Z
dc.date 2008-05-19T09:30:58Z
dc.date 2007-05
dc.date.accessioned 2017-01-31T01:21:48Z
dc.date.available 2017-01-31T01:21:48Z
dc.identifier Peptides 28 (5): 958-968
dc.identifier http://hdl.handle.net/10261/4330
dc.identifier 10.1016/j.peptides.2007.02.014
dc.identifier.uri http://dspace.mediu.edu.my:8181/xmlui/handle/10261/4330
dc.description The definitive verison is available at http://www.sciencedirect.com/science//journal/01969781
dc.description We have identified a family of peptoids that inhibits in vitro the activity of the apoptosome, a macromolecular complex that activates mitochondrial-dependent apoptosis pathways. The analysis of peptide-based cell compatible delivery systems of the most active peptoid is presented. The active peptoid was then fused to cell penetrating peptides (CPP) as penetratin (PEN-peptoid) and HIV-1 TAT (TAT-peptoid). PEN-peptoid showed greater cell viability and as a consequence better efficiency as an apoptosis inhibitor than the TAT-peptoid. The intracellular trafficking of both inhibitors was studied by flow cytometry and confocal fluorescence microscopy. Finally, the influence of the cargo (peptoid) molecules on the conformational behavior of the CPP in buffers and in membrane mimetic environments was analyzed using circular dichroism (CD) spectroscopy.
dc.description This work was supported by grants from Spanish Ministry of Science and Education (MEC) (BIO2004-998 and CTQ2005-00995), Fundación Centro de Investigación Príncipe Felipe and a Marie Curie Reintegration grant (MERG-2004-06307). Mar Orzáez thanks Bancaja for a postdoctoral fellowship. Laura Mondragón is supported by a FPI fellowship from MEC. The confocal microscope was supported by MEC through FEDER.
dc.description Peer reviewed
dc.format 694351 bytes
dc.format application/pdf
dc.language eng
dc.publisher Elsevier
dc.rights openAccess
dc.subject Apoptosis
dc.subject Apoptosome inhibitors
dc.subject Cell-penetrating peptides
dc.subject Drug delivery systems
dc.subject Conformational analysis
dc.subject Membrane mimetics
dc.title Conjugation of a Novel Apaf-1 Inhibitor to Peptide-based Cell-Membrane Transporters. Effective Methods to Improve Inhibition of Mitochondria-Mediated Apoptosis
dc.type Artículo


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