Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/96707
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dc.contributor.authorChen, Hongyuanen
dc.contributor.authorJiao, Wantingen
dc.contributor.authorBickerstaffe, Royen
dc.contributor.authorZvarec, Ondrejen
dc.contributor.authorJones, Matthew A.en
dc.contributor.authorCoxon, James M.en
dc.contributor.authorMorton, James D.en
dc.contributor.authorPehere, Ashok D.en
dc.contributor.authorAbell, Andrew D.en
dc.date.accessioned2013-08-06T03:32:22Zen
dc.date.accessioned2019-12-06T19:34:08Z-
dc.date.available2013-08-06T03:32:22Zen
dc.date.available2019-12-06T19:34:08Z-
dc.date.copyright2012en
dc.date.issued2012en
dc.identifier.citationChen, H., Jiao, W., Jones, M. A., Coxon, J. M., Morton, J. D., Bickerstaffe, R., Pehere, A. D., Zvarec, O.,& Abell, A. D. (2012). New Tripeptide-Based Macrocyclic Calpain Inhibitors Formed by N-Alkylation of Histidine. Chemistry & Biodiversity, 9(11), 2473-2484.en
dc.identifier.issn1612-1872en
dc.identifier.urihttps://hdl.handle.net/10356/96707-
dc.description.abstractTwo new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the peptide backbone are linked by a bridge containing a 1,4-disubstituted 1H-imidazole, are reported. The structure with an aldehyde at the C-terminus and the imidazole at P3, i.e., 4c, shows significant inhibitory activity against calpain 2, with an IC50 value of 238 nM. The macrocyclic aldehyde with the imidazole at the alternative P1 position, i.e., 5c, is significantly less active. The relative activities are linked to the ability of the component macrocycles to mimic a β-strand geometry that is known to favor active-site binding. This ability is defined by conformational searches and docking studies with calpain.en
dc.language.isoenen
dc.relation.ispartofseriesChemistry & biodiversityen
dc.titleNew tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidineen
dc.typeJournal Articleen
dc.contributor.schoolSchool of Materials Science & Engineeringen
dc.identifier.doi10.1002/cbdv.201200320en
item.grantfulltextnone-
item.fulltextNo Fulltext-
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