Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors
- 作者：Tooru Kimura ; Jeffrey-Tri Nguyen ; Hikoichiro Maegawa ; Keiji Nishiyama ; Yasuhiro Arii ; Yasuko Matsui ; Yoshio Hayashi ; Yoshiaki Kiso
- 关键词：Human T-cell leukemia virus ; Adult T-cell leukemia ; Human immunodeficiency virus ; Protease inhibitor
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：15 June 2007
- 卷：17
- 期：12
- 页码：3276-3280
- 文件大小：570 K
摘要
The human T-cell leukemia virus type 1 (HTLV-I) causes adult T-cell leukemia and several severe chronic diseases. HTLV-I protease (PR) inhibition stops the propagation of the virus. Herein, truncation studies were performed on potent octapeptidic HTLV-I PR inhibitor KNI-10161 to derive small hexapeptide KNI-10127 with some loss in activity. After performing residue-substitution studies on compound KNI-10127, HTLV-I PR inhibitory activity was recovered in inhibitor KNI-10166.