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Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors
Authors:Nguyen Jeffrey-Tri  Zhang Meihui  Kumada Henri-Obadja  Itami Ayako  Nishiyama Keiji  Kimura Tooru  Cheng Maosheng  Hayashi Yoshio  Kiso Yoshiaki
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.
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.
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