Short cyclic peptides derived from the C-terminal sequence of α1-antitrypsin exhibit significant anti-HIV-1 activity

Serpin A1 (α1-AT), the largest subgroup of serpins, presents in human plasma at high concentration and plays important regulatory roles in physiological and pathological processes. Accumulated evidence suggests that α1-AT may play a role in controlling HIV-1 Infection. In this study, we designed and synthesized a set of short linear Peptides derived from the C-terminal sequence of α1-AT. Since none of them showed significant anti-HIV-1 activity, we proceeded to synthesize four short cyclic Peptides having 7 Amino acids, and we found that three of them exhibited significant anti-HIV-1 activity. One of these cyclic Peptides, designated CPM, inhibited HIV-1 entry and Infection at low μM level, indicating that these short cyclic Peptides could serve as leads for the development of novel anti-HIV-1 therapeutics.