Polyanionic chemical barriers to HIV-1 binding in CD4 expressing cells (Meeting abstract). NLM AIDSLINE Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

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Polyanionic chemical barriers to HIV-1 binding in CD4 expressing cells (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 36:A1790 1995. Unique Identifier : AIDSLINE ICDB/95609565
Zalkow LH; Burgess EM; Ruell JA; Gruszecka-Kowalik E; Lu H; School of Chemistry and Biochemistry, Georgia Institute of; Technology, Atlanta, GA 30332

Abstract: Using sulfonated azo-dyes as lead compounds, over 125 compounds have been synthesized and screened for their in vitro anti-HIV activity. A QSAR was developed based on electron density distributions and EC50 values. Azo linkages and sulfonic acid residues have been replaced, systematically, by amide linkages and carboxyl residues, respectively, to yield potential drugs with less intense color and better bio-availability. The most promising leads were subjected to computer-simulated docking onto the domain of CD4 recombinant protein to which the virion binds. The results of this investigation have provided a rationale for the design of second generation polyanionic chemical barriers of HIV-1 binding to CD4-expressing cells.
Keywords: Anions Antiviral Agents/*PHARMACOLOGY Cell Line CD4-Positive T-Lymphocytes/*VIROLOGY Human HIV-1/*DRUG EFFECTS Receptors, HIV/*DRUG EFFECTS Structure-Activity Relationship ABSTRACT

KWDanionsantiviralagents/KWDpharmacologycelllinecd4-positivet-lymphocytes/KWDvirologyhumanhiv-1/KWDdrugeffectsreceptors,hiv/KWDdrugeffectsstructure-activityrelationshipabstract
951130
M95B0948

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