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    • 2. 发明申请
    • Peptides as cell penetrating carriers
    • 肽作为细胞穿透载体
    • US20090036363A1
    • 2009-02-05
    • US10591355
    • 2005-03-07
    • Ernest Giralt LledoJimena Fernandez Carneado
    • Ernest Giralt LledoJimena Fernandez Carneado
    • C07K7/06A61K38/16A61K38/10A61K38/08A61K8/64C07K16/46C07K14/00C07K7/08
    • A61K47/42A61K38/00C07K7/06C07K7/08
    • Compounds of formula (I) or their pharmaceutically or biologically acceptable salts are useful as cell penetrating carriers. According to formula (I), below, Val is L-Val or D-Val; Arg is L-Arg, D-Arg or L-(N-methyl)Arg; Pro is L-Pro or D-Pro; Leu is L-Leu or D-Leu; x is an integer from 1 to 20, preferably 3; L1 and L2 are chemical linkers; M1 and M2 are pharmacologically and/or biologically active moieties; and the bond between L1 and M1 and the bond between L2 and M2 are of the known chemical natures, including covalent and ionic. Compared with other previously described carrier peptides, this new family presents several advantages including its non-viral origin, its amphipathic character, its solubility in water and the absence of a cytotoxic effect at high concentrations. M1-L1-(Val-Arg-Leu-Pro-Pro-Pro)x-L2-M2  (I)
    • 式(I)化合物或其药学上或生物可接受的盐可用作细胞穿透载体。 根据下式(I),Val是L-Val或D-Val; Arg是L-Arg,D-Arg或L-(N-甲基)Arg; Pro是L-Pro或D-Pro; Leu是L-Leu或D-Leu; x是1至20的整数,优选3; L1和L2是化学接头; M1和M2是药理学和/或生物活性部分; L1和M1之间的键和L2和M2之间的键是具有已知的化学性质,包括共价键和离子键。 与其他先前描述的载体肽相比,该新家族具有几个优点,包括其非病毒来源,其两亲性特征,其在水中的溶解度和在高浓度下不存在细胞毒性作用。 M1-L1-(Val-Arg-Leu-Pro-Pro-Pro)x-L2-M2(I)<β在线上公式描述=“In-line formula”end =“lead” -line-formula description =“内联公式”end =“tail”?>