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