发明名称 |
Glycosaminoglycan derivatives and their use as inhibitors of tumor invasiveness of metastatic profusion-II |
摘要 |
The present invention comprises a method for impeding the formation of tumor metastasis or tumor invasiveness in a host. Such inhibition comprises administration to the host of a glycosaminoglycan derivative substantially devoid of anticoagulation activity and is an effective inhibitory of heparanase activity. Such a glycosaminoglycan derivative may be provided by purchase or synthesis as directed herein. Parenteral administration to a tumor-bearing host of the glycosaminoglycan derivative results in the exposure of host-borne tumor cells thereto. Such exposure to effective levels of the derivative results in the inhibition of tumor heparanase activity and a lessening of invasiveness and metastatic spread. Heparin, a glycosaminoglycan particularly effective as a heparanase inhibitor and an anti-clotting agent, is a preferred glycosaminoglycan for derivatization. Upon derivatization according to the present invention heparin may be converted into a glycosaminglycan derivative substantially devoid of anticoagulant activity but yet being an effective inhibitor of heparanase activity. Mere reduction of heparin carboxyl groups results in the production of a glycosaminoglycan derivative inhibitory to heparanase activity but without substantially anticoagulant activity non-anticoagulating, heparanase-inhibiting glycosaminoglycan derivatives may also be prepared from heparin, for example, by: at least partial N-desulfation and then N-acetylation; or N-, O-desulfation followed by N-resulfation.
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申请公布号 |
US5262403(A) |
申请公布日期 |
1993.11.16 |
申请号 |
US19900550827 |
申请日期 |
1990.07.10 |
申请人 |
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM |
发明人 |
NICOLSON, GARTH L.;IRIMURA, TATSURO;NAKAJIMA, MOTOWO |
分类号 |
A61K51/12;C08B37/00;C12N9/24;C12Q1/34;G01N33/573;G01N33/574;(IPC1-7):A61K31/725;C08B37/10 |
主分类号 |
A61K51/12 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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