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    Methods for the Characterisation of Interaction Sites on Target Proteins
    2.
    发明申请
    Methods for the Characterisation of Interaction Sites on Target Proteins 审中-公开
    表征目标蛋白质相互作用位点的方法

    公开(公告)号：US20150105274A1

    公开(公告)日：2015-04-16

    申请号：US14377809

    申请日：2013-02-07

    申请人： Phylogica Limited ,  Cambridge Enterprise Limited

    发明人： Paul Watt ,  Bryn Hardwick ,  Grahame McKenzie ,  Ashok Venkitaraman

    IPC分类号： G01N33/68 ,  C07K14/195 ,  G06F19/16 ,  C40B30/02 ,  C12N15/10 ,  G01N33/50

    CPC分类号： G01N33/6845 ,  C07K14/195 ,  C12N15/1079 ,  G01N33/5041 ,  G01N33/6842 ,  G01N2500/10 ,  G16B15/00 ,  G16B35/00 ,  G16C20/60

    摘要： The present invention relates to improved and integrated methods for the characterisation of an interaction site on a target protein that modulates the phenotype of a mammalian cell, such as a phenotype other than death and/or reduced growth. Such methods of the present invention include those to identify a target protein modulates such a phenotype of a mammalian cell, and optionally to characterise an interaction site on said target protein. Such identification and characterisation methods are useful in the development of research tools and/or therapeutics, such protein/peptide or small molecule therapeutics. Accordingly, the present invention also relates to methods of: identification of a ligand, such as a small molecule ligand, that binds to such a target protein; and identification a compound being a candidate modulator of said phenotype of a mammalian cell. The invention further relates to peptides or proteins, or fragments, variants and/or derivatives thereof) comprising certain amino acid sequences, nucleic acids encoding such peptides or proteins and uses of such peptides or proteins or of such nucleic acids.

    摘要翻译： 本发明涉及用于表征调节哺乳动物细胞的表型的靶蛋白上的相互作用位点的改进和综合方法，例如除死亡和/或减少的生长之外的表型。 本发明的这些方法包括鉴定调节哺乳动物细胞的这种表型的靶蛋白，以及任选地表征所述靶蛋白上的相互作用位点的方法。 这种鉴定和表征方法可用于开发研究工具和/或治疗剂，例如蛋白质/肽或小分子治疗剂。 因此，本发明还涉及以下方法：鉴定与这种靶蛋白结合的配体，如小分子配体; 以及鉴定作为所述哺乳动物细胞表型的候选调节剂的化合物。 本发明还涉及包含某些氨基酸序列的肽或蛋白质或其片段，变体和/或衍生物，编码这些肽或蛋白质的核酸以及这种肽或蛋白质或这种核酸的用途。

    Method of monitoring cellular trafficking of peptides
    3.
    发明申请
    Method of monitoring cellular trafficking of peptides 审中-公开
    监测肽的细胞运输的方法

    公开(公告)号：US20160146786A1

    公开(公告)日：2016-05-26

    申请号：US14898064

    申请日：2014-06-26

    申请人： PHYLOGICA LIMITED

    发明人： Richard Hopkins ,  Katrin Hoffmann ,  Tatjana Heinrich ,  Paula Cunningham ,  Paul Watt ,  Nadia Milech

    IPC分类号： G01N33/50

    CPC分类号： G01N33/5035 ,  C12Q1/25 ,  G01N33/52 ,  G01N33/68 ,  G01N2333/9015 ,  G01N2440/32 ,  G01N2500/10

    摘要： This disclosure provides a method of isolating peptides having cell-penetrating function, wherein the peptides are detected as biotinylated molecules only following their translocation through the cell membrane. The disclosure also provides methods for validating the cell-penetrating function of the peptides, or that may be employed in their own right to isolate such peptides, wherein the peptides are detectable by virtue of their ability to transport a detectable cargo into the cytoplasm, such as a cargo toxin or a fragment of a green fluorescent protein (GFP) that is required for complementation of a functional GFP. The disclosure also provides non-canonical peptides having cell-penetrating function that differ structurally from known CPPs such as TAT, VP22, transportan and penetratin, and that are capable of translocating cell membranes and escaping the endosome. The disclosed peptides have utility in transporting cargo therapeutics and diagnostics into cells.

    摘要翻译： 本公开提供了分离具有细胞穿透功能的肽的方法，其中肽仅在其通过细胞膜的移位后才被检测为生物素化分子。 本公开还提供了用于验证肽的细胞穿透功能的方法，或者可以以其本身的权利来分离这些肽，其中肽可以通过将可检测的货物运输到细胞质中而被检测，例如 作为补充功能性GFP所需的货物毒素或绿色荧光蛋白（GFP）的片段。 本公开还提供了具有细胞穿透功能的非规范肽，其结构不同于已知的CPP，例如TAT，VP22，转运蛋白和穿透素，并且能够移位细胞膜并逃逸内体。 所公开的肽可用于将货物治疗和诊断转运到细胞中。