Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/6834
DC Field | Value | Language |
---|---|---|
dc.contributor | Department of Applied Biology and Chemical Technology | - |
dc.creator | Ziemba, A | - |
dc.creator | Hayes, E | - |
dc.creator | Freeman III, BB | - |
dc.creator | Ye, T | - |
dc.creator | Pizzorno, G | - |
dc.date.accessioned | 2014-12-11T08:25:54Z | - |
dc.date.available | 2014-12-11T08:25:54Z | - |
dc.identifier.issn | 2090-2107 (print) | - |
dc.identifier.issn | 2090-2115 (online) | - |
dc.identifier.uri | http://hdl.handle.net/10397/6834 | - |
dc.language.iso | en | en_US |
dc.publisher | Hindawi Publishing Corporation | en_US |
dc.rights | Copyright © 2011 Amy Ziemba et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. | en_US |
dc.title | Development of an oral form of azacytidine : 2′3′5′ triacetyl-5-azacytidine | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.identifier.volume | 2011 | - |
dc.identifier.doi | 10.1155/2011/965826 | - |
dcterms.abstract | Myelodysplastic syndromes (MDSs) represent a group of incurable stem-cell malignancies which are predominantly treated by supportive care. Epigenetic silencing through promoter methylation of a number of genes is present in poor-risk subtypes of MDS and often predicts transformation to acute myelogenous leukemia (AML). Azacitidine and decitabine, two FDA-approved DNA methyltransferase (DNMT) inhibitors, are able to improve overall response although their oral bioavailability complicates their clinical use. This study evaluated 2′,3′,5′-triacetyl-5-azacitidine (TAC) as a potential prodrug for azacitidine. The prodrug demonstrated significant pharmacokinetic improvements in bioavailability, solubility, and stability over the parent compound. In vivo analyses indicated a lack of general toxicity coupled with significantly improved survival. Pharmacodynamic analyses confirmed its ability to suppress global methylation in vivo. These data indicate that esterified nucleoside derivatives may be effective prodrugs for azacitidine and encourages further investigation of TAC into its metabolism, activity, and possible clinical evaluation. | - |
dcterms.accessRights | open access | en_US |
dcterms.bibliographicCitation | Chemotherapy research and practice, v. 2011, 965826, p.1-9 | - |
dcterms.isPartOf | Chemotherapy research and practice | - |
dcterms.issued | 2011 | - |
dc.identifier.pmid | 22295208 | - |
dc.description.oa | Version of Record | en_US |
dc.identifier.FolderNumber | OA_IR/PIRA | en_US |
dc.description.pubStatus | Published | en_US |
Appears in Collections: | Journal/Magazine Article |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
Ziemba_Oral_Form_Azacytidine.pdf | 1.18 MB | Adobe PDF | View/Open |
Page views
119
Last Week
2
2
Last month
Citations as of Apr 21, 2024
Downloads
121
Citations as of Apr 21, 2024
Google ScholarTM
Check
Altmetric
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.