| 摘要 |
<p>An inhibitor of retroviral proteinase comprises a peptide of the formula: (Z)nX-Y(Z)m wherein X is any naturally occurring amino acid (such as tyrosine or phenylalanine) or modified amino acid; Y is an α-imino acid having a 4-, 6-, 7- or 8-membered ring structure; Z is an α-amino acid; and n and m are independently 0 to 7 when the N- or C-terminal amino acids are carrying free NH2 or carboxyl or amide groups, or when the terminal amino acids are blocked at the NH2 or carboxy end. These peptides serve as substrates for the retroviral proteinases and thereby inhibit retroviral proteinase activity without inhibiting nonretroviral proteolytic enzymes of the same family, that is, aspartic proteinases. The peptides selectively inhibit retroviral proteinases (PR) such as HIV-1 PR, HIV-2 PR and EIAV PR. Pharmaceutical compositions comprising the inhibitor and methods of treatment involving same are included.</p> |
