公开(公告)号：WO1998024474A1

公开(公告)日：1998-06-11

申请号：PCT/DK1997000555

申请日：1997-12-08

Applicant: FONDEN TIL FREMME AF EKSPERIMENTEL CANCERFORSKNING ,  LUND, Leif, Roge ,  DANO, Keld ,  STEPHENS, Ross ,  BRÜNNER, Nils ,  SOLBERG, Helene ,  HOLST-HANSEN, Claus ,  NIELSEN, John, Romer

Inventor： FONDEN TIL FREMME AF EKSPERIMENTEL CANCERFORSKNING

IPC: A61K38/57

CPC classification number: A61K45/06 ,  A61K31/40 ,  A61K38/57 ,  A61K31/195 ,  A61K2300/00

Abstract: The invention pertains to novel methods for preventing or arresting invasive remodelling in mammals by utilising a combination of in vivo inhibition of plasmin and in vivo inhibition of certain other proteolytic enzymes, notably metalloproteases. The method can e.g. be used as a novel alternative to current methods of contraception as well as antifungal and antibacterial treatment. The preferred embodiments relate to treatment and prevention of neoplastic diseases by use of these combinations. Further, the invention relates to novel compositions which comprises a plasmin inhibitor in admixture with an inhibitor of another proteolytic enzyme, preferably an inhibitor of a metalloprotease.

Abstract translation: 本发明涉及通过利用体内抑制纤溶酶和体内抑制某些其它蛋白水解酶，特别是金属蛋白酶的组合来预防或阻止哺乳动物侵入性重塑的新方法。 该方法可以例如 用作当前避孕方法以及抗真菌和抗菌治疗的替代方法。 优选实施方案涉及通过使用这些组合来治疗和预防肿瘤疾病。 此外，本发明涉及新型组合物，其包含与另一种蛋白水解酶（优选金属蛋白酶抑制剂）的抑制剂混合的纤溶酶抑制剂。

公开(公告)号：WO1990012091A1

公开(公告)日：1990-10-18

申请号：PCT/DK1990000090

申请日：1990-04-09

Applicant: CANCERFORSKNINGSFONDET AF 1989 ,  DANO, Keld ,  BLASI, Francesco ,  ROLDAN, Ann, Louring ,  CUBELLIS, Maria, Vittoria ,  MASUCCI, Maria, Teresa ,  APPELLA, Ettore ,  SCHLEUNING, W., D. ,  BEHRENDT, Niels ,  RONNE, Ebbe ,  KRISTENSEN, PETER ,  PÖLLÄNEN, Jari ,  SALONEN, Eeva-Marjatta ,  STEPHENS, Ross, W. ,  TAPIOVAARA, Hannele ,  VAHERI, Antii ,  MOLLER, Lisbeth, Birk ,  ELLIS, Vincent ,  LUND, Leif, Roge ,  PLOUG, Michael ,  PYKE, Charles ,  PATTHY, László

Inventor： CANCERFORSKNINGSFONDET AF 1989

IPC: C12N09/72

CPC classification number: C12N9/6462 ,  A61K38/00 ,  A61K38/1808 ,  A61K38/49 ,  A61K39/3955 ,  C07K14/705 ,  C07K16/28 ,  C07K16/2896 ,  C07K2317/76 ,  C07K2317/77 ,  C12Q1/6886 ,  C12Q2600/118 ,  C12Q2600/158 ,  C12Y304/21073 ,  G01N33/57446 ,  G01N33/86 ,  G01N2333/9723 ,  A61K2300/00

Abstract: Pure human cellular receptor for urokinase plasminogen activator (u-PAR) and forms thereof, including a truncated water-soluble form produced by cleaving or removing a glycosyl-phosphatidylinositol anchor, are provided, as is cDNA for u-PAR. Cell surface plasminogen activation, believed to play an important role in tissue remodelling, particularly during cancer invasion, is inhibited by antibodies against u-PAR and by inactivated analogues of u-PA. In situ hybdridization showed presence of u-PAR mRNA in the invasion front of colon carcinomas, proving the diagnostic utility of the cDNA. Water-soluble u-PAR is useful for inhibition of u-PA catalyzed plasminogen activation in solution.

Abstract translation: 提供了用于尿激酶纤溶酶原激活物（u-PAR）的纯人细胞受体及其形式，包括通过切割或除去糖基 - 磷脂酰肌醇锚点产生的截短的水溶性形式，如u-PAR的cDNA。 被认为在组织重塑中起重要作用的细胞表面纤溶酶原激活，特别是在癌症侵袭期间，被u-PAR抗体和u-PA的灭活类似物所抑制。 原位杂交显示u-PAR mRNA在结肠癌侵袭前的存在，证明了cDNA的诊断效用。 水溶性u-PAR可用于抑制溶液中u-PA催化的纤溶酶原激活。