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Protein peptide conjugates associated with the fucosidase inhibitor receptor and its use in the treatment of liver tumors
Protein peptide conjugates associated with the fucosidase inhibitor receptor and its use in the treatment of liver tumors
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机译:与岩藻糖苷酶抑制剂受体相关的蛋白肽结合物及其在肝肿瘤治疗中的应用
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摘要
A peptide conjugate comprising a receptor-associated protein (RAP) peptide bound to a fucosidase inhibitor, the RAP peptide comprising a polypeptide sequence with at least 80% homology to amino acids 210-319 of RAP of the SEQ ID NO: 1, wherein the fucosidase inhibitor inhibits the activity of alpha-L-fucosidase to cleave fucose residues from glycoproteins and induces the accumulation of glycoprotein-derived oligosaccharides in the lysosome, where the fucosidase inhibitor is selected from the group consisting of L-deoxifuconojirimycin (DFJ), beta-1- C-methyl-deoxyimanojirimycin, beta-1-C-ethyl-deoxyimanojirimycin, beta-1-C-phenyl-deoxyimanojirimycin, acid ((3R, 4R, 5S , 6S) -1-butyl-4,5,6-trihydroxyazepane-3-carboxylic acid (Faz), beta-L-homofucononojirimycin, (1-alpha, 2-beta, 3- alpha or beta, 4-alpha, 5- alpha or beta) -2,3,4-trihydroxy-5- (hydroxymethyl) -cyclopentylamines substituted and 2,6-imino-2,6,7-trideoxy-D-glycerol-D-gluco-heptite l.
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机译:一种肽缀合物,其包含与岩藻糖苷酶抑制剂结合的受体相关蛋白(RAP)肽,该RAP肽包含与SEQ ID NO:1的RAP氨基酸210-319具有至少80%同源性的多肽序列。岩藻糖苷酶抑制剂抑制α-L-岩藻糖苷酶从糖蛋白上裂解岩藻糖残基的活性,并诱导糖蛋白衍生的寡糖在溶酶体中的积累,其中岩藻糖苷酶抑制剂选自L-脱氧核糖核酸刀豆霉素(DFJ),β- 1-C-甲基-脱氧金刚霉素,β-1-C-乙基-脱氧金刚霉素,β-1-C-苯基-脱氧金刚霉素,酸((3R,4R,5S,6S)-1-丁基-4,5,6-三羟基氮杂环庚烷-3-羧酸(Faz),β-L-高铁链龙on霉素(1-α,2-β,3-α或β,4-α,5-α或β)-2,3,4-三羟基-取代了5-(羟甲基)-环戊基胺和2,6-亚氨基-2,6,7-三苯氧基-D-甘油-D-葡萄糖-庚二酸酯。
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