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Depositordc.contributorHulme, Alison
Funderdc.contributor.otherEPSRC - Engineering and Physical Sciences Research Councilen_UK
Funderdc.contributor.otherCRUK - Cancer Research UK
Data Creatordc.creatorJohnston, Heather
Data Creatordc.creatorBoys, Sarah
Data Creatordc.creatorMakda, Ashraff
Data Creatordc.creatorCarragher, Neil
Data Creatordc.creatorHulme, Alison
Date Accessioneddc.date.accessioned2016-06-06T14:19:52Z
Date Availabledc.date.available2016-07-31T04:15:16Z
Citationdc.identifier.citationJohnston, Heather; Boys, Sarah; Makda, Ashraff; Carragher, Neil; Hulme, Alison. (2016). Naturally Inspired Peptide Leads: Alanine Scanning Reveals an Actin-Targeting Thiazole Analogue of Bisebromoamide, [dataset]. University of Edinburgh. School of Chemistry.. https://doi.org/10.7488/ds/1417.en
Persistent Identifierdc.identifier.urihttp://hdl.handle.net/10283/2022
Persistent Identifierdc.identifier.urihttps://doi.org/10.7488/ds/1417
Dataset Description (abstract)dc.description.abstractSystematic alanine-scanning of the linear peptide bisebromoamide (BBA), isolated from a marine cyanobacterium, is enabled by targeting the solid phase peptide synthesis of thiazole analogues. The synthetic Tz-BBA analogues have comparable cytotoxicity (nM) to bisebromoamide and cellular morphology assays indicate that they target the actin cytoskeleton. Pathway inhibition in human colon tumour (HCT-116) cells has been explored using reverse phase protein array (RPPA) analysis, which shows a dose-dependent response of IRS-1 expression. Alanine-scanning reveals a structural dependence to the cytotoxicity, actin-targeting and pathway inhibition, and allows a new readily-synthesised lead to be proposed.en_UK
Languagedc.language.isoengen_UK
Publisherdc.publisherUniversity of Edinburgh. School of Chemistry.en_UK
Relation (Is Referenced By)dc.relation.isreferencedbyhttps://doi.org/10.1002/cbic.201600435en_UK
Relation (Is Referenced By)dc.relation.isreferencedbyH. J. Johnston, S. K. Boys, A. Makda, N. O. Carragher, A. N. Hulme, ChemBioChem 2016, 17, 1580. DOI: 10.1002/cbic.201600435.en
Rightsdc.rightsCreative Commons Attribution 4.0 International Public Licenseen
Subjectdc.subjectnon-ribosomal peptideen_UK
Subjectdc.subjectstructure activity relationshipen_UK
Subjectdc.subjectsolid phase synthesisen_UK
Subjectdc.subjectalanine scanen_UK
Subjectdc.subjectIRS-1en_UK
Subjectdc.subjectF-actinen_UK
Subjectdc.subjectRPPAen_UK
Subject Classificationdc.subject.classificationPhysical Sciences::Bio-organic Chemistryen_UK
Titledc.titleNaturally Inspired Peptide Leads: Alanine Scanning Reveals an Actin-Targeting Thiazole Analogue of Bisebromoamideen_UK
Alternative Titledc.title.alternativeChemBioChem 2016 - Bisebromoamide filesen_UK
Typedc.typedataseten_UK

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