| 摘要 |
There is disclosed an isolated polypeptide and derivatives thereof having protease biological activity for human precursor IL-1beta and for a substrate comprising: <?in-line-formulae description="In-line Formulae" end="lead"?>R<SUB>1</SUB>-Asp-R<SUB>2</SUB>-R<SUB>3 </SUB><?in-line-formulae description="In-line Formulae" end="tail"?> wherein R<SUB>1 </SUB>and R<SUB>3 </SUB>are independently any D or L isomer amino acid, R<SUB>2 </SUB>is Ala or Gly, and wherein the specific protease cleavage site is between Asp and R<SUB>2</SUB>. Inhibitor compounds, compositions and methods for inhibiting Interleukin 1beta protease activity are also disclosed. The inhibitor compounds comprise an amino acid sequence of from 1 to about 5 amino acids having an N-terminal blocking group and a C-terminal Asp residue connected to an electronegative leaving group, wherein the amino acid sequence corresponds to the sequence Ala-Tyr-Val-His-Asp.
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