Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties |
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Authors: | Zhang Meihui Nguyen Jeffrey-Tri Kumada Henri-Obadja Kimura Tooru Cheng Maosheng Hayashi Yoshio Kiso Yoshiaki |
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Institution: | 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 causative agent behind adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy is the human T-cell leukemia virus type 1 (HTLV-I). Tetrapeptidic HTLV-I protease inhibitors were designed on a previously reported potent inhibitor KNI-10516, with modifications at the P(3)-cap moieties. All the inhibitors showed high HIV-1 protease inhibitory activity (over 98% inhibition at 50nM) and most exhibited highly potent inhibition against HTLV-I protease (IC(50) values were less than 100nM). |
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