Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.
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.
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.
Meihui
M
Zhang
Jeffrey-Tri
JT
Nguyen
Henri-Obadja
HO
Kumada
Tooru
T
Kimura
Maosheng
M
Cheng
Yoshio
Y
Hayashi
Yoshiaki
Y
Kiso
D015490:HTLV-I Infections / Q000188:drug therapy; D015368:Human T-lymphotropic virus 1 / Q000201:enzymology*; D006801:Humans; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D010455:Peptides; D011480:Protease Inhibitors