Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.
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.
Nguyen
Jeffrey-Tri
JT
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.
Zhang
Meihui
M
Kumada
Henri-Obadja
HO
Itami
Ayako
A
Nishiyama
Keiji
K
Kimura
Tooru
T
Cheng
Maosheng
M
Hayashi
Yoshio
Y
Kiso
Yoshiaki
Y
D019943:Amino Acid Substitution; D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology*; D015368:Human T-lymphotropic virus 1 / Q000201:enzymology*; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D000596:Amino Acids; D009842:Oligopeptides; D011480:Protease Inhibitors