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    • 2. 发明申请
    • CELL-PENETRATING PEPTIDES AND USES THEROF
    • 细胞穿刺肽及其用途
    • WO2011157713A4
    • 2012-04-12
    • PCT/EP2011059853
    • 2011-06-14
    • HOFFMANN LA ROCHEBRINKMANN ULRICHHAAS ALEXANDERMAISEL DANIELA
    • BRINKMANN ULRICHHAAS ALEXANDERMAISEL DANIELA
    • A61K47/48C07K14/00
    • C07K14/47A61K47/6455C07K1/1075C07K1/1077C07K14/00C07K14/435
    • The present invention relates to a peptide molecule capable of being internalized into a cell, wherein the peptide molecule (a) has a length of at least 10, preferably of at least 15 amino acid residues; (b) comprises in its primary amino acid sequence at least 25%, preferably at least 30% positively charged amino acid residues; and (c) is internalized into a cell with an efficacy being at least 80%, preferably at least 90% of the internalization efficacy of the TAT peptide having the amino acid sequence GRKKRRQRRRPPQ. The invention is also directed to a corresponding nucleic acid molecule encoding such peptide as well as to a composition comprising at least one such peptide being attached to any one of the group consisting of one or more nucleic acid molecules, one or more peptides or proteins, one or more small molecules, and one or more nanoparticles, wherein the attachment is accomplished by a linkage selected from the group consisting of a covalent linkage and a non-covalent linkage. Furthermore, the invention relates to a method of detecting the internalization behavior of such peptide or such composition, comprising (a) administering the peptide or composition to one or more cells; and (b) detecting the internalization of the peptide or composition. Finally, the invention concerns the use of such peptide or such composition for the transformation or transfection of one or more cells as well as in the prevention and/or treatment of a condition selected from the group consisting of cancer, immune diseases, cardiovascular diseases, neuronal diseases, infections, and inflammatory diseases.
    • 本发明涉及能够内化到细胞中的肽分子,其中肽分子(a)的长度至少为10,优选至少15个氨基酸残基; (b)在其主要氨基酸序列中包含至少25%,优选至少30%带正电荷的氨基酸残基; 并且(c)被内化成细胞,其功效为具有氨基酸序列GRKKRRQRRRPPQ的TAT肽的内在功效的至少80%,优选至少90%。 本发明还涉及编码这种肽的相应核酸分子以及包含至少一种这样的肽的组合物,其连接到由一种或多种核酸分子,一种或多种肽或蛋白质组成的组中的任何一种, 一种或多种小分子和一种或多种纳米颗粒,其中所述连接通过选自共价键和非共价键的键进行。 此外,本发明涉及检测这种肽或这种组合物的内化行为的方法,其包括(a)将肽或组合物施用于一种或多种细胞; 和(b)检测肽或组合物的内在化。 最后,本发明涉及这样的肽或这种组合物用于转化或转染一种或多种细胞以及预防和/或治疗选自以下的病症:癌症,免疫疾病,心血管疾病, 神经元疾病,感染和炎性疾病。
    • 3. 发明申请
    • CELL-PENETRATING PEPTIDES AND USES THEROF
    • 细胞渗透肽及其应用
    • WO2011157713A3
    • 2012-02-23
    • PCT/EP2011059853
    • 2011-06-14
    • HOFFMANN LA ROCHEBRINKMANN ULRICHHAAS ALEXANDERMAISEL DANIELA
    • BRINKMANN ULRICHHAAS ALEXANDERMAISEL DANIELA
    • A61K47/48C07K14/00
    • C07K14/47A61K47/6455C07K1/1075C07K1/1077C07K14/00C07K14/435
    • The present invention relates to a peptide molecule capable of being internalized into a cell, wherein the peptide molecule (a) has a length of at least 10, preferably of at least 15 amino acid residues; (b) comprises in its primary amino acid sequence at least 25%, preferably at least 30% positively charged amino acid residues; and (c) is internalized into a cell with an efficacy being at least 80%, preferably at least 90% of the internalization efficacy of the TAT peptide having the amino acid sequence GRKKRRQRRRPPQ. The invention is also directed to a corresponding nucleic acid molecule encoding such peptide as well as to a composition comprising at least one such peptide being attached to any one of the group consisting of one or more nucleic acid molecules, one or more peptides or proteins, one or more small molecules, and one or more nanoparticles, wherein the attachment is accomplished by a linkage selected from the group consisting of a covalent linkage and a non-covalent linkage. Furthermore, the invention relates to a method of detecting the internalization behavior of such peptide or such composition, comprising (a) administering the peptide or composition to one or more cells; and (b) detecting the internalization of the peptide or composition. Finally, the invention concerns the use of such peptide or such composition for the transformation or transfection of one or more cells as well as in the prevention and/or treatment of a condition selected from the group consisting of cancer, immune diseases, cardiovascular diseases, neuronal diseases, infections, and inflammatory diseases.
    • 本发明涉及能够被内化到细胞中的肽分子,其中肽分子(a)具有至少10个,优选至少15个氨基酸残基的长度; (b)在其一级氨基酸序列中包含至少25%,优选至少30%带正电的氨基酸残基; 和(c)以具有氨基酸序列GRKKRRQRRRPPQ的TAT肽的内化效力的至少80%,优选至少90%的效力内化到细胞中。 本发明还涉及编码此类肽的相应核酸分子以及包含至少一个此类肽的组合物,所述组合物连接至由一个或多个核酸分子,一个或多个肽或蛋白质组成的组中的任何一个, 一个或多个小分子和一个或多个纳米颗粒,其中所述连接通过选自共价键和非共价键的键实现。 此外,本发明涉及检测此类肽或此类组合物的内化行为的方法,其包括(a)将所述肽或组合物给予一种或多种细胞; 和(b)检测肽或组合物的内化。 最后,本发明涉及这种肽或这种组合物用于转化或转染一种或多种细胞以及预防和/或治疗选自癌症,免疫疾病,心血管疾病, 神经元疾病,感染和炎症性疾病。