Document Detail


Telomerase inhibition, telomere shortening, and decreased cell proliferation by cell permeable 2'-O-methoxyethyl oligonucleotides.
MedLine Citation:
PMID:  12459009     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Telomerase is an attractive target for chemotherapy. Testing this hypothesis will require potent inhibitors with favorable pharmacokinetic properties. We report that 2'-methoxyethyl oligonucleotides complementary to the telomerase RNA component diffuse across cell membranes without the need for cationic carrier lipid, inhibit telomerase, and cause telomeres to shorten. The ability of antitelomerase oligomers to enter cells without the need to add lipid will simplify preclinical studies and may suggest advantages for clinical use.
Authors:
Zhi Chen; Brett P Monia; David R Corey
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  45     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2002 Dec 
Date Detail:
Created Date:  2002-12-02     Completed Date:  2003-01-07     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  5423-5     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas 75390-9041, USA.
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MeSH Terms
Descriptor/Qualifier:
Cell Division / drug effects
Cell Membrane Permeability
Enzyme Inhibitors / chemical synthesis*,  chemistry,  pharmacology
Humans
Oligonucleotides / chemical synthesis*,  chemistry,  pharmacology
Structure-Activity Relationship
Telomerase / antagonists & inhibitors*
Tumor Cells, Cultured
Grant Support
ID/Acronym/Agency:
CA70907/CA/NCI NIH HHS; CA85363/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Oligonucleotides; EC 2.7.7.49/Telomerase

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


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