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Interleukin 1β protease and interleukin 1β protease inhibitors

机译:白介素1β蛋白酶和白介素1β蛋白酶抑制剂

摘要

There is disclosed an isolated polypeptide and derivatives thereof having protease biological activity for human precursor IL-1β 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 1β 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.
机译:公开了一种分离的多肽及其衍生物,其对人前体IL-1β和底物具有蛋白酶生物学活性,所述底物包括:<?in-line-formulae description =“ In-line Formulae” end =“ lead”?> R 1 -Asp-R 2 -R 3 < / Sub> <?in-line-formulae description =“在线公式” end =“ tail”?>其中R 1 和R 3 独立地是任何D或L异构体氨基酸,R 2 是Ala或Gly,并且其中特定的蛋白酶裂解站点位于Asp和R 2 之间。还公开了抑制白介素1β蛋白酶活性的抑制剂化合物,组合物和方法。抑制剂化合物包含具有N端封闭基团和连接至负电离去基团的C端Asp残基的1至约5个氨基酸的氨基酸序列,其中该氨基酸序列对应于序列Ala-Tyr- Val-His-Asp。

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