Kazuo Kumagai

Increased anti‐HIV‐1 activity of CD4 CDR3‐related synthetic peptides by scrambling and further structural modifications, including d‐isomerization and dimerization

We recently showed that S1, a sequence‐scrambled form of CD4 CDR3‐related synthetic peptide, has more potent inhibitory activities on HIV‐1 replication and HIV‐1‐induced syncytium formation than the original form. In this study, a series of derivatives of S1 were synthesized and their anti‐HIV‐1 activities were evaluated. A d‐isomer was as potent as S1, and a homodimer was 10‐ to 18‐fold more potent than S1. The increased antiviral activity of the dimer peptide was related to α‐helix formation, as detected by circular dichroism.