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ID: ALA1148015

Journal: Bioorg Med Chem Lett

Title: Chipping at large, potent human T-cell leukemia virus type 1 protease inhibitors to uncover smaller, equipotent inhibitors.

Authors: Kimura T, Nguyen JT, Maegawa H, Nishiyama K, Arii Y, Matsui Y, Hayashi Y, Kiso Y.

Abstract: 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.

CiteXplore: 17448657

DOI: 10.1016/j.bmcl.2007.04.019