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    • 62. 发明公开
    • MODIFICATIONS OF PEPTIDE COMPOSITIONS TO INCREASE STABILITY AND DELIVERY EFFICIENCY
    • 变形金刚PEPTIDZUSAMMENSETZUNGENFÜRERHÖHTESTABILITÄTUND AUSGABEEFFIZIENZ
    • EP2109619A2
    • 2009-10-21
    • EP08728081.4
    • 2008-01-22
    • Kai Pharmaceuticals, Inc.
    • MACLEAN, Derek
    • C07K14/00
    • C12N9/96A61K38/10A61K47/64A61K47/645C07K7/00C12N9/12C12Y207/11013
    • The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A "therapeutic peptide composition" comprises a "carrier peptide" and a "cargo peptide." A "carrier peptide" is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The "cargo peptide" is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.
    • 所公开的发明涉及改进肽组合物以提高稳定性和递送效率的方法。 具体地,所公开的发明涉及增加蛋白激酶C(PKC)调节肽组合物的稳定性和递送效率的方法。 “治疗性肽组合物”包含“载体肽”和“货物肽”。“载体肽”是促进细胞摄取治疗性肽组合物的肽内的肽或氨基酸序列。 “货物肽”是PKC调节肽。 通过减少二硫键交换,物理稳定性,减少蛋白水解降解和提高细胞摄取效率,本文所述的肽载体肽,载体肽或两者的肽修饰增加了治疗性肽组合物的稳定性和递送效率。