公开(公告)号：US20060008464A1

公开(公告)日：2006-01-12

申请号：US10508959

申请日：2003-04-03

申请人： Chaim Gilon ,  Abraham Loyter ,  Adolf Graessman ,  Ilana Hariton-Gazal ,  Joseph Sperling

发明人： Chaim Gilon ,  Abraham Loyter ,  Adolf Graessman ,  Ilana Hariton-Gazal ,  Joseph Sperling

IPC分类号： A61K39/00 ,  C07K14/47

CPC分类号： A61K47/645 ,  A61K47/62 ,  A61K47/643

摘要： A conjugate of a histone moiety covalently attached to a macromolecule-of-interest, in which the histone moiety is transportable through the cell membrane and importable into the cell nuclei, is disclosed. Further disclosed are chemical and recombinant methods of preparing such a conjugate, pharmaceutical compositions containing same and uses thereof for delivering therapeutically active macromolecules into cells. A novel method for quantitatively determining a cytoplasmic uptake and/or a nuclear uptake of a moiety into cells is also disclosed.

摘要翻译： 公开了共价连接到感兴趣的大分子的组蛋白部分的缀合物，其中组蛋白部分可通过细胞膜传输并可导入细胞核。 进一步公开的是制备这种缀合物的化学和重组方法，含有它的药物组合物和用于将治疗活性大分子递送到细胞中的用途。 还公开了用于定量测定部分细胞的细胞质摄取和/或核摄取的新方法。