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Título

Peptide-biphenyl hybrids as calpain inhibitors

AutorMontero, Ana; Mann, Enrique ; Chana López, Antonio ; Herradón García, Bernardo
Fecha de publicación25-mar-2004
EditorJohn Wiley & Sons
CitaciónChemistry & Biodiversity 1(3): 442-457 (2004)
ResumenCalpain is a cysteine protease that is activated by Ca2+. The over-activation of calpain, which occurs on increasing Ca2+ concentration, causes a variety of diseases. This paper reports experimental results on the inhibition of calpain I (μ-calpain) by peptide-biphenyl hybrids. We have found that some peptide-biphenyl hybrids, with aromatic amino acids in the peptide chains, inhibit calpain with IC50 values in the nanomolar range. Since the peptide-biphenyl hybrids reported in the present paper do not posses a reactive electrophilic functionality, we hypothesize that they interfere with the activation of calpain by Ca2+, and present experimental and computational results on the binding of peptide-biphenyl hybrids to Ca2+.
Descripción16 pages, 7 figures.-- PMID: 17191858 [PubMed].-- Taken in part from the Ph.D. thesis of A. C. (December, 2003) and the projected Ph.D. thesis of A. M. Spanish patent ES-P200301125 was filed as of Feb 16, 2006.
Versión del editorhttp://dx.doi.org/10.1002/cbdv.200490037
URIhttp://hdl.handle.net/10261/11409
DOI10.1002/cbdv.200490037
ISSN1612-1872 (Print)
1612-1880 (Online)
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