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BIFUNCTIONAL UROCINASE-VARIANTS HAVING IMPROVED FIBRINOLYTIC PROPERTIES AND THROMBIN-INHIBITING ACTIVITY

机译:具有改善的纤溶特性和凝血酶抑制活性的功能性尿素酶变种

摘要

Bifunctional space kinase variants with improved fibrinolytic lytic needle degeneration and throbin inhibitory activity, plasmids for use in the preparation of these polypeptides, and single-bifunctional space kinase variants containing the active ingredient are added to the trypticolytic enzymes. The bifunctional space kinase variants of the present invention correspond to the general formula (I), wherein M4 is as defined in FIG. Figure 47A shows the amino acid sequence of the non-glycosylated prebase kinase 47Ser and 411Leβ; X1 is a bond between M4 and Y1, or a Ser-Pro-Pro-Pro-Ser-Pro-Pro-Gly-Gly-Ser-Pro-Pro-Ser-Pro-Pro-Ser-Pro-Pro-Gly-Gly-PhevagySer -Pro-Pro-Ser-Pro-Pro-Pro-Ser-Pro-Pro-Gly-Gly-Phe-Glycic peptide; or a peptide sequence of general formula (II) wherein X2 is Pro or Leu; X 3 represents Val or Prő; X 4 is Lys, Val, Arg, Gly or Gly; X 5 is Ala, Val, Gly, Leû or Ile; X6 is Phe, Trp, Tyr or Val, and X7 is Gly or a direct bond between X6 and Y1 -; and Y 1 is a Y 2 -Arg-Pr-Y 3 -Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Gly-Gly-Ile-Pr-Gly-Gly-Tyr-Leyl-Y 4; or aY2-Arg-Pr-Phe-Leu-Le-Arg-Asn-Pr-Asn-Asp-Lys-Tyr-Gly-Pr-Phe-Trp-Gly-Asp-Gly-Gly-Lys-Asn-Gly ; or a peptide of the general formula Y 2 -Arg-Pr-Ser-Ser-Gly-Phe-Gly-Gly-Phe-Gly-Ile-Asp-Gly-Gly-Gly-Gly-Lys, wherein Y 2 is Pr or Val; Y3 is Leu or a direct bond between Pro and Gly, and Y4 is Gln or hydroxy tube. ŕ
机译:将具有改善的纤溶蛋白裂解针变性和纤溶蛋白抑制活性的双功能性空间激酶变体,用于制备这些多肽的质粒和含有活性成分的单双功能性空间激酶变体添加到类胰蛋白酶中。本发明的双功能空间激酶变体对应于通式(I),其中M4如在图1中所定义。图47A显示了非糖基化的前碱基激酶47Ser和411Leβ的氨基酸序列。 X1是M4和Y1之间的键,或者是Ser-Pro-Pro-Pro-Pro-Ser-Pro-Pro-Gly-Gly-Ser-Pro-Pro-Ser-Pro-Pro-Ser-Pro-Pro-Gly-Gly -PhevagySer -Pro-Pro-Ser-Pro-Pro-Pro-Ser-Pro-Pro-Gly-Gly-Phe-甘氨酸肽;或通式(II)的肽序列,其中X 2是Pro或Leu; X 3代表Val或Prő; X 4为Lys,Val,Arg,Gly或Gly; X 5为Ala,Val,Gly,Leû或Ile; X6是Phe,Trp,Tyr或Val,X7是Gly或X6和Y1-之间的直接键。 Y 1为Y 2 -Arg-Pr-Y 3 -Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Gly-Gly-Ile-Pr-Gly-Gly-Tyr-Leyl-Y 4。或aY2-Arg-Pr-Phe-Leu-Le-Arg-Asn-Pr-Asn-Asp-Lys-Tyr-Gly-Pr-Phe-Trp-Gly-Asp-Gly-Gly-Lys-Asn-Gly或通式Y 2-Arg-Pr-Ser-Ser-Gly-Phe-Gly-Gly-Phe-Gly-Ile-Asp-Gly-Gly-Gly-Gly-Lys的肽,其中Y 2为Pr或Val; Y3是Leu或Pro和Gly之间的直接键,Y4是Gln或羟基管。 ŕ

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