Peptide HIV-1 integrase inhibitors from HIV-1 gene products.
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.
Suzuki
Shintaro
S
Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kandasurugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
Urano
Emiko
E
Hashimoto
Chie
C
Tsutsumi
Hiroshi
H
Nakahara
Toru
T
Tanaka
Tomohiro
T
Nakanishi
Yuta
Y
Maddali
Kasthuraiah
K
Han
Yan
Y
Hamatake
Makiko
M
Miyauchi
Kosuke
K
Pommier
Yves
Y
Beutler
John A
JA
Sugiura
Wataru
W
Fuji
Hideyoshi
H
Hoshino
Tyuji
T
Itotani
Kyoko
K
Nomura
Wataru
W
Narumi
Tetsuo
T
Yamamoto
Naoki
N
Komano
Jun A
JA
Tamamura
Hirokazu
H
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*
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