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    • 3. 发明申请
    • Interleukin 1beta protease and interleukin 1beta protease inhibitors
    • 白介素1beta蛋白酶和白细胞介素1β蛋白酶抑制剂
    • US20060188474A1
    • 2006-08-24
    • US11213530
    • 2005-08-25
    • Paul SleathRoy BlackShirley Kronheim
    • Paul SleathRoy BlackShirley Kronheim
    • A61K38/20C07K14/545C07H21/04C12P21/04
    • C12N9/6475A61K38/00C12N9/6421
    • 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.
    • 公开了一种分离的多肽及其衍生物,其对于人前体IL-1β和底物具有蛋白酶生物学活性,其包含:<?in-line-formula description =“In-line formula”end =“lead”?> R 1-in-line-formula description =“In-line Formulas”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,并且其中特异性蛋白酶裂解 位于Asp和R 2 2之间。 还公开了抑制白细胞介素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-末端封闭基团的1至约5个氨基酸的氨基酸序列和与电负离子基团连接的C末端Asp残基,其中氨基酸序列对应于序列Ala-Tyr- Val-His-Asp。