Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies

dc.contributor.authorYelekçi, Kemal
dc.contributor.authorDayangac-Erden, Didem
dc.contributor.authorDemir, Ayhan S.
dc.contributor.authorDalkara, Sevim
dc.contributor.authorYelekçi, Kemal
dc.contributor.authorErdem-Yurter, Hayat
dc.date.accessioned2019-06-27T08:05:37Z
dc.date.available2019-06-27T08:05:37Z
dc.date.issued2009
dc.departmentFakülteler, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümüen_US
dc.description.abstractIn the light of known HDAC inhibitors 33 carboxylic acid derivatives were tested to understand the structural requirements for HDAC inhibition activity. Several modifications were applied to develop the structure-activity relationships of carboxylic acid HDAC inhibitors. HDAC inhibition activities were investigated in vitro by using HeLa nuclear extract in a fluorimetric assay. Molecular docking was also carried out for the human HDAC8 enzyme in order to predict inhibition activity and the 3D poses of inhibitor-enzyme complexes. Of these compounds caffeic acid derivatives such as chlorogenic acid and curcumin were found to be highly potent compared to sodium butyrate which is a well-known HDAC inhibitor. (C) 2009 Elsevier Ltd. All rights reserved.en_US]
dc.identifier.citation145
dc.identifier.doi10.1016/j.bmc.2009.05.042en_US
dc.identifier.endpage5228
dc.identifier.issn0968-0896en_US
dc.identifier.issn1464-3391en_US
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.issue14
dc.identifier.pmid19520580en_US
dc.identifier.scopus2-s2.0-67650078931en_US
dc.identifier.scopusqualityQ2
dc.identifier.startpage5219en_US
dc.identifier.urihttps://hdl.handle.net/20.500.12469/1096
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2009.05.042
dc.identifier.volume17en_US
dc.identifier.wosWOS:000267873000044en_US
dc.identifier.wosqualityQ2
dc.institutionauthorYelekçi, Kemalen_US
dc.language.isoenen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.relation.journalBioorganic & Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectHDAC inhibitorsen_US
dc.subjectMolecular dockingen_US
dc.subjectCaffeic acid derivativesen_US
dc.subjectChlorogenic aciden_US
dc.subjectCurcuminen_US
dc.subjectCarboxylic acid derivativesen_US
dc.titleMolecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studiesen_US
dc.typeArticleen_US
dspace.entity.typePublication
relation.isAuthorOfPublication9407938e-3d31-453b-9199-aaa8280a66c5
relation.isAuthorOfPublication.latestForDiscovery9407938e-3d31-453b-9199-aaa8280a66c5

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