Benzopurpurin and related compounds inhibit the binding of gp120 to galactosyl ceramide/sulfatide and infection of human immunodeficiency virus.
In an attempt to find compounds capable of inhibiting the binding and infection by human immunodeficiency virus type 1 (HIV-1) in neural cells, we studied the effect of benzopurpurin and related compounds on the binding of gp120 to galactosyl ceramide (GalCer) and sulfatide. In this report, we show that the binding of gp120 to GalCer and sulfatide is inhibited by benzopurpurin and related compounds. These compounds also inhibit the binding and entry of HIV-1 to neural cell line, SK-N-MC. Binding studies indicate that benzopurpurin and related compounds bind to gp120. Studies involving related compounds indicate that the minimal structure required for the inhibition is two naphthalene rings with amine or sulfonic acids attached to a central biphenyl molecule by an azo group. This approach will be useful for screening of potential anti-HIV compounds.
Bhat
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Department of Neurology, University of Pennyslvania Medical Center, Philadelphia, PA 19104.
Otsuka
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Srinivasan
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D000998:Antiviral Agents / Q000494:pharmacology*; D002460:Cell Line; D005699:Galactosylceramides / Q000378:metabolism*; D015699:HIV Envelope Protein gp120 / Q000187:drug effects* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D015394:Molecular Structure; D009282:Naphthalenesulfonates / Q000494:pharmacology*; D009474:Neurons / Q000166:cytology / Q000382:microbiology; D011485:Protein Binding / Q000187:drug effects; D013433:Sulfoglycosphingolipids / Q000378:metabolism*; D014779:Virus Replication
D000998:Antiviral Agents; D005699:Galactosylceramides; D015699:HIV Envelope Protein gp120; D009282:Naphthalenesulfonates; D013433:Sulfoglycosphingolipids; C007060:benzopurpurine 4B