Abstract
The causative agent behind adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy is the human T-cell leukemia virus type 1 (HTLV-I). Tetrapeptidic HTLV-I protease inhibitors were designed on a previously reported potent inhibitor KNI-10516, with modifications at the P(3)-cap moieties. All the inhibitors showed high HIV-1 protease inhibitory activity (over 98% inhibition at 50nM) and most exhibited highly potent inhibition against HTLV-I protease (IC(50) values were less than 100nM).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aspartic Acid Endopeptidases / antagonists & inhibitors*
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Binding Sites
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Dose-Response Relationship, Drug
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Drug Evaluation, Preclinical
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HIV Protease / drug effects
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Humans
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Inhibitory Concentration 50
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Models, Molecular
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Molecular Conformation
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Oligopeptides
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Protease Inhibitors
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Aspartic Acid Endopeptidases
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HIV Protease
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HTLV-1 protease
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p16 protease, Human immunodeficiency virus 1