Molecular Modifications on Carboxylic Acid Derivatives as Potent Histone Deacetylase Inhibitors: Activity and Docking Studies
| dc.contributor.author | Bora-Tatar, Gamze | |
| dc.contributor.author | Dayangac-Erden, Didem | |
| dc.contributor.author | Demir, Ayhan S. | |
| dc.contributor.author | Dalkara, Sevim | |
| dc.contributor.author | Yelekçi, Kemal | |
| dc.contributor.author | Erdem-Yurter, Hayat | |
| dc.date.accessioned | 2019-06-27T08:05:37Z | |
| dc.date.available | 2019-06-27T08:05:37Z | |
| dc.date.issued | 2009 | |
| dc.description.abstract | In 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.doi | 10.1016/j.bmc.2009.05.042 | en_US |
| dc.identifier.issn | 0968-0896 | |
| dc.identifier.issn | 1464-3391 | |
| dc.identifier.scopus | 2-s2.0-67650078931 | en_US |
| dc.identifier.uri | https://hdl.handle.net/20.500.12469/1096 | |
| dc.identifier.uri | https://doi.org/10.1016/j.bmc.2009.05.042 | |
| dc.language.iso | en | en_US |
| dc.publisher | Pergamon-Elsevier Science Ltd | en_US |
| dc.relation.ispartof | Bioorganic & Medicinal Chemistry | |
| dc.rights | info:eu-repo/semantics/openAccess | en_US |
| dc.subject | HDAC inhibitors | en_US |
| dc.subject | Molecular docking | en_US |
| dc.subject | Caffeic acid derivatives | en_US |
| dc.subject | Chlorogenic acid | en_US |
| dc.subject | Curcumin | en_US |
| dc.subject | Carboxylic acid derivatives | en_US |
| dc.title | Molecular Modifications on Carboxylic Acid Derivatives as Potent Histone Deacetylase Inhibitors: Activity and Docking Studies | en_US |
| dc.type | Article | en_US |
| dspace.entity.type | Publication | |
| gdc.author.institutional | Yelekçi, Kemal | en_US |
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| gdc.coar.access | open access | |
| gdc.coar.type | text::journal::journal article | |
| gdc.collaboration.industrial | false | |
| gdc.description.department | Fakülteler, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümü | en_US |
| gdc.description.endpage | 5228 | |
| gdc.description.issue | 14 | |
| gdc.description.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
| gdc.description.scopusquality | Q2 | |
| gdc.description.startpage | 5219 | en_US |
| gdc.description.volume | 17 | en_US |
| gdc.description.wosquality | Q1 | |
| gdc.identifier.openalex | W1964757070 | |
| gdc.identifier.pmid | 19520580 | en_US |
| gdc.identifier.wos | WOS:000267873000044 | en_US |
| gdc.index.type | WoS | |
| gdc.index.type | Scopus | |
| gdc.index.type | PubMed | |
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| gdc.oaire.keywords | Models, Molecular | |
| gdc.oaire.keywords | Curcumin | |
| gdc.oaire.keywords | Molecular Structure | |
| gdc.oaire.keywords | Carboxylic Acids | |
| gdc.oaire.keywords | Chlorogenic acid | |
| gdc.oaire.keywords | Histone Deacetylases | |
| gdc.oaire.keywords | Histone Deacetylase Inhibitors | |
| gdc.oaire.keywords | Carboxylic acid derivatives | |
| gdc.oaire.keywords | Caffeic Acids | |
| gdc.oaire.keywords | HDAC inhibitors | |
| gdc.oaire.keywords | Catalytic Domain | |
| gdc.oaire.keywords | Molecular docking | |
| gdc.oaire.keywords | Humans | |
| gdc.oaire.keywords | Caffeic acid derivatives | |
| gdc.oaire.keywords | Chlorogenic Acid | |
| gdc.oaire.keywords | Enzyme Inhibitors | |
| gdc.oaire.keywords | HeLa Cells | |
| gdc.oaire.keywords | Protein Binding | |
| gdc.oaire.popularity | 4.851891E-8 | |
| gdc.oaire.publicfunded | false | |
| gdc.oaire.sciencefields | 0301 basic medicine | |
| gdc.oaire.sciencefields | 0303 health sciences | |
| gdc.oaire.sciencefields | 03 medical and health sciences | |
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| gdc.opencitations.count | 165 | |
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| gdc.relation.journal | Bioorganic & Medicinal Chemistry | |
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| gdc.virtual.author | Yelekçi, Kemal | |
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