Document Detail


Aryloxy phosphoramidate triesters: a technology for delivering monophosphorylated nucleosides and sugars into cells.
MedLine Citation:
PMID:  19760699     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Prodrug technologies aimed at delivering nucleoside monophosphates into cells (protides) have proved to be effective in improving the therapeutic potential of antiviral and anticancer nucleosides. In these cases, the nucleoside monophosphates are delivered into the cell, where they may then be further converted (phosphorylated) to their active species. Herein, we describe one of these technologies developed in our laboratories, known as the phosphoramidate protide method. In this approach, the charges of the phosphate group are fully masked to provide efficient passive cell-membrane penetration. Upon entering the cell, the masking groups are enzymatically cleaved to release the phosphorylated biomolecule. The application of this technology to various therapeutic nucleosides has resulted in improved antiviral and anticancer activities, and in some cases it has transformed inactive nucleosides to active ones. Additionally, the phosphoramidate technology has also been applied to numerous antiviral nucleoside phosphonates, and has resulted in at least three phosphoramidate-based nucleotides progressing to clinical investigations. Furthermore, the phosphoramidate technology has been recently applied to sugars (mainly glucosamine) in order to improve their therapeutic potential. The development of the phosphoramidate technology, mechanism of action and the application of the technology to various monophosphorylated nucleosides and sugars will be reviewed.
Authors:
Youcef Mehellou; Jan Balzarini; Christopher McGuigan
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  ChemMedChem     Volume:  4     ISSN:  1860-7187     ISO Abbreviation:  ChemMedChem     Publication Date:  2009 Nov 
Date Detail:
Created Date:  2009-10-29     Completed Date:  2010-01-28     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101259013     Medline TA:  ChemMedChem     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  1779-91     Citation Subset:  IM    
Affiliation:
Cardiff University, UK. mcguigan@cardiff.ac.uk
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MeSH Terms
Descriptor/Qualifier:
Amides / chemistry*,  pharmacology
Anti-HIV Agents / chemistry,  pharmacology
Antineoplastic Agents / chemistry,  pharmacology
Antiviral Agents / chemistry,  pharmacology
Carbohydrates / chemistry*,  pharmacology
Cell Line, Tumor
Drug Carriers
Humans
Nucleosides / chemistry*,  pharmacology
Phosphoric Acids / chemistry*,  pharmacology
Chemical
Reg. No./Substance:
0/Amides; 0/Anti-HIV Agents; 0/Antineoplastic Agents; 0/Antiviral Agents; 0/Carbohydrates; 0/Drug Carriers; 0/Nucleosides; 0/Phosphoric Acids; 2817-45-0/phosphoramidic acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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