Antiviral/Peptides: Synthetic Peptides that Prevent HIV from Binding to CD4

Summary

Novelty: The patent discloses a composition of chemically modified human CD4 antigen, consisting of derivatized peptides having substantially the same core seven-amino-acid sequence (of N-terminal proximal sequences) with at least one amino acid side-chain modified. It is useful as a vaccine and inhibitor of retrovirus-induced cell fusion, virion infectivity and virus transmission.

Biology: The activity of derivatized CD4 is illustrated by a large number of test results including inhibition of HIV-1 and HIV-2 infection of CEM-SS cells by CD4 (74092) post-resin peptide mixture, HTLV-IIIB Vn/Vo² = 0.003 to 0.78, HIV-2 Vn/Vo = 0.1 to greater than 1.0 at a peptide concentration 2 to 250 μM; inhibition of HIV-induced cell fusion by CD4 derived synthetic peptide composition, potency = 16 to greater than 500 μM and purity = 57% to 100%; inhibition of HIV fusion assay by T₁C₄E₅ tribenzyl CD4 (81-92) derivatives, IC₁₀₀ = 16 to 50 μM.