Document Detail


Specific CD4 down-modulating compounds with potent anti-HIV activity.
MedLine Citation:
PMID:  12960237     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Despite the availability of the current clinically approved anti-HIV drugs, new classes of effective antiviral agents are still urgently needed to combat AIDS. A promising approach for drug development and vaccine design involves targeting research on HIV-1 entry, a multistep process that comprises viral attachment, coreceptor interactions, and fusion. Determination of the viral entry process in detail has enabled the design of specific agents that can inhibit each step in the HIV entry process. Therapeutic agents that interfere with the binding of the HIV envelope glycoprotein gp120 to the CD4 receptor (e.g., PRO 542, PRO 2000, and CV-N) or the coreceptors CCR5 and CXCR4 (e.g., SCH-C and AMD3100) are briefly outlined in this review. The anti-HIV activity of cyclotriazadisulfonamides, a novel class of compounds with a unique mode of action by down-modulating the CD4 receptor in lymphocytic and monocytic cells, is especially highlighted. On the basis of the successful results of T-20, the first approved entry inhibitor, the development of effective antiretrovirals that block HIV entry will certainly be further encouraged.
Authors:
Kurt Vermeire; Dominique Schols
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2003-08-01
Journal Detail:
Title:  Journal of leukocyte biology     Volume:  74     ISSN:  0741-5400     ISO Abbreviation:  J. Leukoc. Biol.     Publication Date:  2003 Nov 
Date Detail:
Created Date:  2003-11-03     Completed Date:  2004-01-09     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8405628     Medline TA:  J Leukoc Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  667-75     Citation Subset:  IM    
Affiliation:
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium.
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MeSH Terms
Descriptor/Qualifier:
Anti-HIV Agents / pharmacology*,  therapeutic use
Antigens, CD4 / drug effects*
Cell Line
HIV Envelope Protein gp120 / drug effects
HIV-1 / drug effects,  physiology*
Humans
Lymphocytes / immunology
Monocytes / immunology
Receptors, HIV / physiology
Chemical
Reg. No./Substance:
0/Anti-HIV Agents; 0/Antigens, CD4; 0/HIV Envelope Protein gp120; 0/Receptors, HIV

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