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Methods of affecting intracellular phosphorylation of tyrosine using phosphorothioate oligonucleotides, and antiangiogenic and antiproliferative uses thereof
Methods of affecting intracellular phosphorylation of tyrosine using phosphorothioate oligonucleotides, and antiangiogenic and antiproliferative uses thereof
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机译:使用硫代磷酸酯寡核苷酸影响酪氨酸胞内磷酸化的方法及其抗血管生成和抗增殖用途
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摘要
The present invention provides methods of stimulating or inhibiting intracellular phosphorylation of tyrosine by a heparin- binding receptor which comprises contacting a cell having on its surface the heparin- binding receptor with a phosphorothioate oligonucleotide moiety of suitable length and base composition, such phosphorothioate oligonucleotide moiety being present in an effective amount. The invention further provides a method of inhibiting the formation of blood vessels in a subject which comprises administering to the subject an amount of a phosphorothioate oligonucleotide moiety of suitable length and base composition. The invention also provides a method of inhibiting proliferation of cells having a malignant phenotype in a subject which comprises administering to the subject an amount of a phosphorothioate oligonucleotide moiety of suitable length and base composition.
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机译: 6.一种化合物,其包含具有根据20的EP-B1-2563920(SEQ ID NO:80)的具有由20个连接的核苷组成的核碱基序列的修饰的寡核苷酸,其中所述修饰的寡核苷酸包含:由十个连接的脱氧核苷组成的缺口片段;和由五个连接的核苷组成的5'翼区段; 3'翼段由五个连接的核苷组成;其中所述间隙片段位于5'侧翼片段和3'侧翼片段之间,其中每个侧翼片段的每个核苷包含2'-O-甲氧基乙基糖;其中修饰的寡核苷酸的每个胞嘧啶是5-甲基胞嘧啶,并且其中修饰的寡核苷酸的每个核苷间键是硫代磷酸酯键;特别是inotersen;及其衍生物,例如由EP-B1-2563920保护的其盐,包括钠盐。