C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 15/57 (2006.01) A61K 38/04 (2006.01) A61K 38/48 (2006.01) C07C 271/22 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) C07K 7/06 (2006.01) C07K 14/545 (2006.01) C12N 9/64 (2006.01) C12N 15/24 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2111100
There is disclosed an isolated polypeptide and derivatives thereof having protease biological activity for human precursor IL=1.beta. and for a substrate comprising: R1-Asp-R2-R3 wherein R1 and R3 are independently any D or L isomer amino acid, R2 is Ala or Gly, and wherein the specific protease cleavage site is between Asp and R2. Inhibitor compounds; compositions and methods for inhibiting Interleukin 1.beta. 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.
Black Roy A.
Kronheim Shirley R.
Sleath Paul R.
Fetherstonhaugh & Co.
Sterling Winthrop Inc.
Vertex Pharmaceuticals Incorporated
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