发明名称 OPIORPHIN PEPTIDE DERIVATIVES AS POTENT INHIBITORS OF ENKEPHALIN-DEGRADING ECTOPEPTIDASES
摘要 The present invention relates to modified opiorphin peptides as new inhibitors of metallo-ectopeptidases.
申请公布号 US2015065683(A1) 申请公布日期 2015.03.05
申请号 US201414537929 申请日期 2014.11.11
申请人 INSTITUT PASTEUR 发明人 ROUGEOT Catherine
分类号 C07K7/06 主分类号 C07K7/06
代理机构 代理人
主权项 1. A peptide derivative of formula (I): ζ-AA1-AA2-AA3-AA4-AA5-OH  (I), wherein: ζ is hydrogen atom, tyrosine, Y-[linker]- or a Zn chelating group, such as a cysteine, C-[linker], N-acetyl-cysteine, N-mercaptoacetyl (HS—CH2—CO—), hydroxamic acid (HO—NH—CO—) or an optionally substituted hydroxyquinoline,AA1 is Q or Glp,AA2 is K, R or H, preferably R,AA3 is Y, G, N, F or F(X), preferably F or F(X),AA4 is P, S or S(OAlk), preferably S or S(OAlk),AA5 is K or R, preferably R,C-[linker]- meaning Cys-[NH—(CH2)n-CO]—, wherein n is an integer between 1 and 20,Y-[linker]- meaning Tyr-[NH—(CH2)n′—CO]—, wherein n′ is an integer between 1 and 20,F(X) meaning a phenylalanine, the phenyl group of which is substituted by one or more halogen atoms,S(OAlk) meaning a serine, the hydroxyl group of which is substituted by a linear or branched alkanoyl group having from 1 to 20 carbon atoms,said AA1, AA2, AA3, AA4, and AA5 are independently either in the L-configuration or D-configuration, and any one of AA1, AA2, AA3, AA4, and AA5 may be optionally a β amino acid, an aza-amino acid or a β-aza-amino acid; wherein if the peptide derivative comprises a cysteine, said peptide derivative is optionally a dimer, with the proviso that the peptide is not QRSFR, QHNPR, QRGPR, YQRFSR or GlpRFSR.
地址 Paris FR