Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/118429
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dc.contributor.authorPehere, A.D.en
dc.contributor.authorNguyen, S.en
dc.contributor.authorGarlick, S.K.en
dc.contributor.authorWilson, D.W.en
dc.contributor.authorHudson, I.en
dc.contributor.authorSykes, M.J.en
dc.contributor.authorMorton, J.D.en
dc.contributor.authorAbell, A.D.en
dc.date.issued2019en
dc.identifier.citationBioorganic and Medicinal Chemistry, 2019; 27(2):436-441en
dc.identifier.issn0968-0896en
dc.identifier.issn1464-3391en
dc.identifier.urihttp://hdl.handle.net/2440/118429-
dc.description.abstractThe 26S proteasome and calpain are linked to a number of important human diseases. Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor MG132 that show a unique combination of high activity and selectivity for calpains over proteasome. Tripeptide aldehydes (1-3) with an aromatic P3 substituent show enhanced activity and selectivity against ovine calpain 2 relative to chymotrypsin-like activity of proteasome. Docking studies reveal the key contacts between inhibitors and calpain to confirm the importance of the S3 pocket with respect to selectivity between calpains 1 and 2 and the proteasome.en
dc.description.statementofresponsibilityAshok D. Pehere, Steven Nguyen, Sarah K. Garlick, Danny W. Wilson, Irene Hudson, Matthew J. Sykes, James D. Morton, Andrew D. Abellen
dc.language.isoenen
dc.publisherElsevieren
dc.rights© 2018 Elsevier Ltd. All rights reserved.en
dc.subjectCalpain inhibitors; 26S proteasome inhibitors; peptidomimetics; medicinal chemistryen
dc.titleTripeptide analogues of MG132 as protease inhibitorsen
dc.typeJournal articleen
dc.identifier.rmid0030106095en
dc.identifier.doi10.1016/j.bmc.2018.12.022en
dc.identifier.pubid453745-
pubs.library.collectionBiochemistry publicationsen
pubs.library.teamDS14en
pubs.verification-statusVerifieden
pubs.publication-statusPublisheden
dc.identifier.orcidWilson, D.W. [0000-0002-5073-1405]en
dc.identifier.orcidAbell, A.D. [0000-0002-0604-2629]en
Appears in Collections:Biochemistry publications

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