title: Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies.
abstract: Structure-activity relationship studies were conducted on HIV integrase (IN) inhibitory peptides which were found by the screening of an overlapping peptide library derived from HIV-1 gene products. Since these peptides located in the second helix of Vpr are considered to have an alpha-helical conformation, Glu-Lys pairs were introduced into the i and i+4 positions to increase the helicity of the lead compound possessing an octa-arginyl group. Ala-scan was also performed on the lead compound for the identification of the amino acid residues responsible for the inhibitory activity. The results indicated the importance of an alpha-helical structure for the expression of inhibitory activity, and presented a binding model of integrase and the lead compound.
authors: Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
authors: Shintaro
authors: S
authors: Suzuki
authors: Kasthuraiah
authors: K
authors: Maddali
authors: Chie
authors: C
authors: Hashimoto
authors: Emiko
authors: E
authors: Urano
authors: Nami
authors: N
authors: Ohashi
authors: Tomohiro
authors: T
authors: Tanaka
authors: Taro
authors: T
authors: Ozaki
authors: Hiroshi
authors: H
authors: Arai
authors: Hiroshi
authors: H
authors: Tsutsumi
authors: Tetsuo
authors: T
authors: Narumi
authors: Wataru
authors: W
authors: Nomura
authors: Naoki
authors: N
authors: Yamamoto
authors: Yves
authors: Y
authors: Pommier
authors: Jun A
authors: JA
authors: Komano
authors: Hirokazu
authors: H
authors: Tamamura
mesh_terms: D000595:Amino Acid Sequence; D002460:Cell Line; D002942:Circular Dichroism; D018698:Glutamic Acid / Q000737:chemistry; D019428:HIV Integrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008239:Lysine / Q000737:chemistry; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D054325:vpr Gene Products, Human Immunodeficiency Virus / Q000737:chemistry*
chemical_list: D019428:HIV Integrase Inhibitors; D010455:Peptides; D054325:vpr Gene Products, Human Immunodeficiency Virus; C514912:vpr protein, Human immunodeficiency virus 1; D018698:Glutamic Acid; D008239:Lysine