title: Peptide HIV-1 integrase inhibitors from HIV-1 gene products.
abstract: Anti-HIV peptides with inhibitory activity against HIV-1 integrase (IN) have been found in overlapping peptide libraries derived from HIV-1 gene products. In a strand transfer assay using IN, inhibitory active peptides with certain sequential motifs related to Vpr- and Env-derived peptides were found. The addition of an octa-arginyl group to the inhibitory peptides caused a remarkable inhibition of the strand transfer and 3'-end-processing reactions catalyzed by IN and significant inhibition against HIV replication.
authors.affiliation: Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
authors.forename: Shintaro
authors.initials: S
authors.lastname: Suzuki
authors.forename: Emiko
authors.initials: E
authors.lastname: Urano
authors.forename: Chie
authors.initials: C
authors.lastname: Hashimoto
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tsutsumi
authors.forename: Toru
authors.initials: T
authors.lastname: Nakahara
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Tanaka
authors.forename: Yuta
authors.initials: Y
authors.lastname: Nakanishi
authors.forename: Kasthuraiah
authors.initials: K
authors.lastname: Maddali
authors.forename: Yan
authors.initials: Y
authors.lastname: Han
authors.forename: Makiko
authors.initials: M
authors.lastname: Hamatake
authors.forename: Kosuke
authors.initials: K
authors.lastname: Miyauchi
authors.forename: Yves
authors.initials: Y
authors.lastname: Pommier
authors.forename: John A
authors.initials: JA
authors.lastname: Beutler
authors.forename: Wataru
authors.initials: W
authors.lastname: Sugiura
authors.forename: Hideyoshi
authors.initials: H
authors.lastname: Fuji
authors.forename: Tyuji
authors.initials: T
authors.lastname: Hoshino
authors.forename: Kyoko
authors.initials: K
authors.lastname: Itotani
authors.forename: Wataru
authors.initials: W
authors.lastname: Nomura
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Narumi
authors.forename: Naoki
authors.initials: N
authors.lastname: Yamamoto
authors.forename: Jun A
authors.initials: JA
authors.lastname: Komano
authors.forename: Hirokazu
authors.initials: H
authors.lastname: Tamamura
mesh_terms: D000595:Amino Acid Sequence; D002460:Cell Line; D045744:Cell Line, Tumor; D005814:Genes, Viral; D019427:HIV Integrase / Q000737:chemistry; D019428:HIV Integrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics* / Q000502:physiology; D054298:Human Immunodeficiency Virus Proteins / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D019151:Peptide Library; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects; D054299:env Gene Products, Human Immunodeficiency Virus / Q000737:chemistry*; D054325:vpr Gene Products, Human Immunodeficiency Virus / Q000737:chemistry*
chemical_list: D019428:HIV Integrase Inhibitors; D054298:Human Immunodeficiency Virus Proteins; D019151:Peptide Library; D010455:Peptides; D054299:env Gene Products, Human Immunodeficiency Virus; D054325:vpr Gene Products, Human Immunodeficiency Virus; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1