Zhang Meihui, Nguyen Jeffrey-Tri, Kumada Henri-Obadja, Kimura Tooru, Cheng Maosheng, Hayashi Yoshio, Kiso Yoshiaki
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.
Bioorg Med Chem. 2008 Jul 15;16(14):6880-90. doi: 10.1016/j.bmc.2008.05.052. Epub 2008 May 28.
Adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy are only some of the more common end results of an infection with a human T-cell leukemia virus type 1 (HTLV-I). Expanding from our previous reports, we synthesized all different permutations of tetrapeptidic HTLV-I protease inhibitors using at least eight P(3)-cap and five P(1)(')-cap moieties. The inhibitors exhibited over 97% inhibition against HIV-1 protease and a wide range of inhibitory activity against HTLV-I protease.
成人T细胞白血病和热带痉挛性截瘫/HTLV-I相关脊髓病只是感染1型人类T细胞白血病病毒（HTLV-I）较为常见的部分最终结果。在我们之前报告的基础上进行拓展，我们使用至少8种P(3)-帽和5种P(1)'-帽部分合成了四肽HTLV-I蛋白酶抑制剂的所有不同排列形式。这些抑制剂对HIV-1蛋白酶的抑制率超过97%，并且对HTLV-I蛋白酶具有广泛的抑制活性。
