Document Detail

Inhibitors of HIV-1 replication [corrected; erratum to be published] that inhibit HIV integrase.
MedLine Citation:
PMID:  8692814     Owner:  NLM     Status:  MEDLINE    
HIV-1 replication depends on the viral enzyme integrase that mediates integration of a DNA copy of the virus into the host cell genome. This enzyme represents a novel target to which antiviral agents might be directed. Three compounds, 3,5-dicaffeoylquinic acid, 1-methoxyoxalyl-3,5-dicaffeoylquinic acid, and L-chicoric acid, inhibit HIV-1 integrase in biochemical assays at concentrations ranging from 0.06-0.66 microgram/ml; furthermore, these compounds inhibit HIV-1 replication in tissue culture at 1-4 microgram/ml. The toxic concentrations of these compounds are fully 100-fold greater than their antiviral concentrations. These compounds represent a potentially important new class of antiviral agents that may contribute to our understanding of the molecular mechanisms of viral integration. Thus, the dicaffeoylquinic acids are promising leads to new anti-HIV therapeutics and offer a significant advance in the search for new HIV enzyme targets as they are both specific for HIV-1 integrase and active against HIV-1 in tissue culture.
W E Robinson; M G Reinecke; S Abdel-Malek; Q Jia; S A Chow
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Proceedings of the National Academy of Sciences of the United States of America     Volume:  93     ISSN:  0027-8424     ISO Abbreviation:  Proc. Natl. Acad. Sci. U.S.A.     Publication Date:  1996 Jun 
Date Detail:
Created Date:  1996-08-23     Completed Date:  1996-08-23     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7505876     Medline TA:  Proc Natl Acad Sci U S A     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  6326-31     Citation Subset:  IM; X    
Department of Pathology, University of California, Irvine 92717-4800, USA.
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MeSH Terms
Antiviral Agents / pharmacology*
Base Sequence
Caffeic Acids*
Cell Line
Chlorogenic Acid / analogs & derivatives*,  pharmacology
DNA Nucleotidyltransferases / antagonists & inhibitors*
Enzyme Inhibitors / pharmacology
HIV-1 / enzymology,  physiology*
Molecular Sequence Data
Succinates / pharmacology*
Virus Replication / drug effects*
Grant Support
Reg. No./Substance:
0/1-methoxyoxalyl-3,5-dicaffeoylquinic acid; 0/3,5-dicaffeoylquinic acid; 0/Antiviral Agents; 0/Caffeic Acids; 0/Enzyme Inhibitors; 0/Oligodeoxyribonucleotides; 0/Succinates; 327-97-9/Chlorogenic Acid; 70831-56-0/chicoric acid; EC 2.7.7.-/DNA Nucleotidyltransferases; EC 2.7.7.-/Integrases

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

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