公开(公告)号：US4844897A

公开(公告)日：1989-07-04

申请号：US906240

申请日：1986-09-12

申请人： Hiroshi Maeda ,  Yasuhiro Matsumura ,  Osamu Asami ,  Hideyuki Tanaka ,  Ikuharu Sasaki

发明人： Hiroshi Maeda ,  Yasuhiro Matsumura ,  Osamu Asami ,  Hideyuki Tanaka ,  Ikuharu Sasaki

IPC分类号： A61K38/00 ,  C12N9/52 ,  C12N9/54 ,  C12N9/96

CPC分类号： C12N9/54 ,  C12N9/52 ,  C12N9/96 ,  A61K38/00

摘要： Method of treating a tumor in a mammal comprises administering to said mammal an effective anti-tumor amount of proteases originating from microorganisms.Method of treating a tumor in a mammal comprises administering to said mammal an effective anti-tumor amount of a protease originating from a microorganism which protease is chemically modified by one of the following procedures:(a) coupling with a saccharide,(b) introduction of a hydrophobic polymeric group,(c) alteration of electric charge of the protein surface,(d) conjugation with a low molecular weight anti-tumor agent of molecular weight less than 2,000,(e) formation of dimer or oligomer by cross-linking of protease molecules,(f) conjugation with a synthetic polycation,(g) conjugation with a synthetic polyanion, and(h) combination of the above-mentioned procedures.Microorganism protease is chemically modified by one of the following procedures:(a) coupling with a saccharide,(b) introduction of a hydrophobic polymeric group,(c) alteration of electric charge of the protein surface,(d) conjugation with a low molecular weight anti-tumor agent of molecular weight less than 2,000,(e) formation of dimer or oligomer by cross-linking of protease molecules,(f) conjugation with a synthetic polycation,(g) conjugation with a synthetic polyanion, and(h) combination of the above-mentioned procedures.

摘要翻译： 治疗哺乳动物肿瘤的方法包括向所述哺乳动物施用有效的抗肿瘤量的源于微生物的蛋白酶。 治疗哺乳动物肿瘤的方法包括向所述哺乳动物施用有效的抗肿瘤量的来自微生物的蛋白酶，所述蛋白酶通过以下方法之一进行化学修饰：（a）与糖的偶联，（b）引入 的疏水性聚合物组，（c）蛋白质表面电荷的改变，（d）与分子量小于2,000的低分子量抗肿瘤剂缀合，（e）通过交联形成二聚体或低聚物 的蛋白酶分子，（f）与合成聚阳离子的缀合，（g）与合成聚阴离子的缀合，和（h）上述步骤的组合。 微生物蛋白酶通过以下方法之一进行化学修饰：（a）与糖的偶联，（b）引入疏水聚合基团，（c）改变蛋白质表面的电荷，（d）与低分子 （e）通过蛋白酶分子的交联形成二聚体或寡聚体，（f）与合成聚阳离子的缀合，（g）与合成聚阴离子的缀合，和（h）分子量小于2000的重量抗肿瘤剂， 组合上述程序。