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ACTIVELY TRANSPORTED AND PROTEASE-RESISTANT PEPTIDES AS BBB SHUTTLES AND SHUTTLE-CARGO CONSTRUCTS

机译:积极运输和抗蛋白酶抗性肽作为BBB梭和班车组建

摘要

It is described a peptidic compound having in its structure a biradical of a peptide having 9-20 amino acids residues in length having at least a intrapeptide disulfide bond, a intrapeptide amide bond, an intrapeptide thioether bond, a Se-Se bond, an intrapeptide C-C bond, or an intrapeptide C=C bond; and comprising the amino acid sequence Xaa 1KAPETALXaa 2 (A)n1(A)n2(A)n3 (SEQ ID NO:1) Xaa 1 and Xaa 2 are an amino acid independently selected form C, D, E, K, O, Dap, Dab, Sec, Pen, AIGly, and alpha-Me-alpha-alkGly; n1, n2 and n3 are integers independently selected from 0 an 1, with the proviso that when at least one of n1, n2 and n3 is 0, then at least an intrapeptide bond is between Xaa 1 and Xaa 2.These peptidic compounds are useful as shuttles through the blood brain barrier (BBB). The constructs BBB-shuttle-cargo, being the cargo of a biologically active substance or for use in a diagnostic method, are useful in therapy and diagnosis.
机译:描述了一种肽化合物,其在其结构中具有9-20个氨基酸残基的肽,其长度具有至少具有脑啡肽二硫键,腹腔内酰胺键,腹腔内键,脑内粘合剂,脑内粘合剂 CC键,或腹腔内C = C键; 并包含氨基酸序列XAA 1KapetalXAA 2(A)N1(A)N 2(A)N 2(A)N 3(SEQ ID NO:1)XAA 1和XAA 2是独立地选择的氨基酸C,D,E,K,O, dap,dab,sec,笔,aigly和alpha-me-alpha-alkly; N1,N2和N3是独立地选择的整数,其具有0α1的整数,具有诸如N1,N 2和N 3中的至少一个为0时,至少在XAA 1和XAA 2.这些肽化合物之间是有用的 通过血脑屏障(BBB)穿梭。 构建BBB-Shuttle-Cargo,作为生物活性物质的货物或用于诊断方法,可用于治疗和诊断。

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