Document Detail


Novel short oligonucleotide conjugates as inhibitors of human telomerase.
MedLine Citation:
PMID:  14565482     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of oligonucleotide conjugates were designed and synthesized as novel inhibitors of human telomerase. These compounds contain a relatively short (6-7-mer) oligonucleotide domain, with an N3'-->P5' phosphoramidate (np) or thio-phosphoramidate (nps) backbone, targeted to the template region of the RNA component of the enzyme and various pendant groups attached to either their 5'- or preferably to the 3'-termini. The most potent compounds in the series inhibited telomerase with low nM IC50 values in biochemical assays whereas the cognate oligonucleotides without the pendant groups were significantly less active having IC50 values 100-1000-fold higher.
Authors:
Krisztina Pongracz; Shihong Li; Brittney-Shea Herbert; Ronald Pruzan; Ellen Wunder; Allison Chin; Mieczyslaw Piatyszek; Jerry Shay; Sergei M Gryaznov
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Nucleosides, nucleotides & nucleic acids     Volume:  22     ISSN:  1525-7770     ISO Abbreviation:  Nucleosides Nucleotides Nucleic Acids     Publication Date:    2003 May-Aug
Date Detail:
Created Date:  2003-10-20     Completed Date:  2003-12-11     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  100892832     Medline TA:  Nucleosides Nucleotides Nucleic Acids     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1627-9     Citation Subset:  IM    
Affiliation:
Geron Corporation, Menlo Park, California 94025, USA. kpongracz@geron.com
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MeSH Terms
Descriptor/Qualifier:
Amides
Base Sequence
Enzyme Inhibitors / chemical synthesis*,  pharmacology
Fluorescent Dyes
Humans
Oligodeoxyribonucleotides / chemical synthesis*,  pharmacology
Phosphoric Acids
Structure-Activity Relationship
Telomerase / antagonists & inhibitors*
Chemical
Reg. No./Substance:
0/Amides; 0/Enzyme Inhibitors; 0/Fluorescent Dyes; 0/Oligodeoxyribonucleotides; 0/Phosphoric Acids; 2817-45-0/phosphoramidic acid; EC 2.7.7.49/Telomerase

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


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