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Fusion peptide intended for inhibition of the interaction of a neural NMDA receptor (NMDAR) with protein interacting with NMDAR
Fusion peptide intended for inhibition of the interaction of a neural NMDA receptor (NMDAR) with protein interacting with NMDAR
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机译:用于抑制神经NMDA受体(NMDAR)与与NMDAR相互作用的蛋白质相互作用的融合肽
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摘要
1. A fusion peptide containing at least component (I), where component (I) is a transporting peptide and component (II) selected from peptides having the ability to inhibit the interaction of a neural N-methyl-D-aspartate receptor (NMDAR) with interacting with NMDAR proteins, where component (II) consists entirely of D-enantiomeric amino acids. ! 2. The fusion peptide according to claim 1, in which component (I) is selected from peptides that have the ability to penetrate into the cell, including:! (a) protein transduction domains (PTDs) and derived from CPP protein, including sequences derived from the genome of flies carrying the Antennapedia mutation, pAntp (43-58), which contain the sequences RQIKIWFQNRRMKWKK (SEQ ID NO: 1) or RQIKIWFQNRRMKKKK SEQ ID NO: 2); including sequences derived from human immunodeficiency virus 1 (HIV-1), Tat, region 37-72, region 37-60, region 48-60 or region 49-57 from TAT, sequences GRKKRRQRRR (SEQ ID NO: 3), YGRKKRRQRRR (SEQ ID NO: 4), CGRKKRRQRRRRPPQC (SEQ ID NO: 5) or CGRKKRRQRRRRPPQCC (SEQ ID NO: 6); including hCT (9-32) having the sequence LGTYTQDFNKFHTFPQTAIGVGAP-NH2 (SEQ ID NO: 7); pVEC containing the sequence LLIILRRRIRKQAHAHSK-NH2 (SEQ ID NO: 8); pISL containing the sequence RVIRVWFQNKRCKDKK-NH2 (SEQ ID NO: 9); murine PRP (1-28) containing the sequence MANGLYWLLALFVTMWTDVGLCKKRPKP-NH2 (SEQ ID NO: 10) or their homologues, including human homologues; Ems (194-220) containing the sequence RQGAARVTSWLGLQLRIAGKRLEGRSK-NH2 (SEQ ID NO: 11); Restricocin L3 (60-73) containing the sequence KLIKGRTPIKFGK-NH2 (SEQ ID NO: 12) or! (b) model peptides, including VT5, containing the sequence DPKGDPKGVTVTVTVTVTGKGDPKPD-NH2 (SEQ ID NO: 13), a MAP containing the sequence KLALKLALKALKAALKLA-NH2 (SEQ ID NO: 14), arginine segments, including RRRRRRR, i.e. (Arg) 7 (SEQ ID NO: 15), or RRRRRRRR-NH2, i.e. (Arg) 7-NH2 (SEQ ID NO: 16), or RRRRRRRR-C, i.e. (
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机译:1.一种至少包含组分(I)的融合肽,其中组分(I)是转运肽,并且组分(II)选自具有抑制神经N-甲基-D-天冬氨酸受体(NMDAR)相互作用的能力的肽)与NMDAR蛋白相互作用,其中组分(II)完全由D对映体氨基酸组成。 ! 2.根据权利要求1的融合肽,其中组分(I)选自具有穿透细胞能力的肽,包括: (a)源于CPP蛋白的蛋白转导域(PTD),包括来源于携带天线突变pAntp(43-58)的苍蝇基因组的序列,其序列包含RQIKIWFQNRRMKWKK(SEQ ID NO:1)或RQIKIWFQNRRMKKKK SEQ编号:2);包括源自人免疫缺陷病毒1(HIV-1),Tat,TAT的区域37-72,区域37-60,区域48-60或区域49-57的序列,序列GRKKRRQRRR(SEQ ID NO:3),YGRKKRRQRRR( SEQ ID NO:4),CGRKKRRQRRRRPPQC(SEQ ID NO:5)或CGRKKRRQRRRRPPQQCC(SEQ ID NO:6);包括具有序列LGTYTQDFNKFHTFPQTAIGVGAP-NH2(SEQ ID NO:7)的hCT(9-32);含有序列LLIILRRRIRKQAHAHSK-NH2(SEQ ID NO:8)的pVEC; pISL,其包含序列RVIRVWFQNKRCKDKKK-NH2(SEQ ID NO:9);含有序列MANGLYWLLALFVTMWTDVGLCKKRPKP-NH2(SEQ ID NO:10)或其同源物(包括人同源物)的鼠PRP(1-28);含有序列RQGAARVTSWLGLQLRIAGKRLEGRSK-NH2(SEQ ID NO:11)的Ems(194-220);含有序列KLIKGRTPIKFGK-NH2(SEQ ID NO:12)的Restricocin L3(60-73)或! (b)包含VT5的模型肽,其包含序列DPKGDPKGVTVTVTVTVTGTGGDPKPD-NH2(SEQ ID NO:13),包含序列KLALKLALKALKAALKLA-NH2(SEQ ID NO:14)的MAP,精氨酸片段,包括RRRRRRR,即(Arg)7 (SEQ ID NO:15),或RRRRRRRR-NH2,即(Arg)7-NH2(SEQ ID NO:16),或RRRRRRRR-C,即(
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