title: Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.
abstract: The culprit behind adult T-cell leukemia, myelopathy/tropical paraparesis, and a plethora of inflammatory diseases is the human T-cell leukemia virus type 1 (HTLV-I). We recently unveiled a potent hexapeptidic HTLV-I protease inhibitor, KNI-10166, composed mostly of natural amino acid residues. Herein, we report the derivation of potent tetrapeptidic inhibitor KNI-10516, possessing only non-natural amino acid residues.
authors.affiliation: Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science and 21st Century COE Program, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
authors.forename: Jeffrey-Tri
authors.initials: JT
authors.lastname: Nguyen
authors.forename: Meihui
authors.initials: M
authors.lastname: Zhang
authors.forename: Henri-Obadja
authors.initials: HO
authors.lastname: Kumada
authors.forename: Ayako
authors.initials: A
authors.lastname: Itami
authors.forename: Keiji
authors.initials: K
authors.lastname: Nishiyama
authors.forename: Tooru
authors.initials: T
authors.lastname: Kimura
authors.forename: Maosheng
authors.initials: M
authors.lastname: Cheng
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Hayashi
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Kiso
mesh_terms: D019943:Amino Acid Substitution; D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology*; D015368:Human T-lymphotropic virus 1 / Q000201:enzymology*; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000596:Amino Acids; D009842:Oligopeptides; D011480:Protease Inhibitors