title: Short cyclic peptides derived from the C-terminal sequence of α1-antitrypsin exhibit significant anti-HIV-1 activity.
abstract: 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.
authors.affiliation: Beijing Institute of Pharmacology & Toxicology, Pharmaceutical Chemistry, 27 Taiping Road, Beijing 100850, China.
authors.forename: Qiyan
authors.initials: Q
authors.lastname: Jia
authors.forename: Xifeng
authors.initials: X
authors.lastname: Jiang
authors.forename: Fei
authors.initials: F
authors.lastname: Yu
authors.forename: Jiayin
authors.initials: J
authors.lastname: Qiu
authors.forename: Xiaoyu
authors.initials: X
authors.lastname: Kang
authors.forename: Lifeng
authors.initials: L
authors.lastname: Cai
authors.forename: Lin
authors.initials: L
authors.lastname: Li
authors.forename: Weiguo
authors.initials: W
authors.lastname: Shi
authors.forename: Shuwen
authors.initials: S
authors.lastname: Liu
authors.forename: Shibo
authors.initials: S
authors.lastname: Jiang
authors.forename: Keliang
authors.initials: K
authors.lastname: Liu
mesh_terms: D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D017434:Protein Structure, Tertiary; D013601:T-Lymphocytes / Q000187:drug effects / Q000821:virology; D053586:Virus Internalization / Q000187:drug effects; D014779:Virus Replication / Q000187:drug effects; D000515:alpha 1-Antitrypsin / Q000737:chemistry*
chemical_list: D019380:Anti-HIV Agents; D010456:Peptides, Cyclic; D000515:alpha 1-Antitrypsin