التفاصيل البيبلوغرافية
| العنوان: |
Peptide Inhibitors of Matrix Metalloproteinase Activity |
| Document Number: |
20070207967 |
| تاريخ النشر: |
September 6, 2007 |
| Appl. No: |
11/578793 |
| Application Filed: |
April 21, 2005 |
| مستخلص: |
The present invention relates to novel matrix metalloproteinase (MMP) inhibitors and down-regulators, to pharmaceutical compositions comprising these inhibitors/down-regulators, to the improvement of liposome targeting to cancer cells, to the use of the novel MMP inhibitors for the manufacture of pharmaceutical and research preparations, to a method for inhibiting and down-regulating MMP-dependent conditions either in vivo or in vitro, to a method for inhibiting activations and/or functions as well catalytic and non-catalytic actions of matrix metalloproteinases, and to the use of the novel MMP inhibitors and down-regulators in biochemical isolation and purification procedures of matrix metalloproteinases. |
| Inventors: |
Bjorklund, Mikael (Helsinki, FI); Koivunen, Erkki (Helsinki, FI) |
| Assignees: |
CTT CANCER TARGETING TECHNOLOGIES OY (Helsinki, FI) |
| Claim: |
1. A matrix metalloproteinase inhibitor and down-regulator comprising the structure of the peptide motif CRXYGPXXXC (SEQ ID NO: 3) wherein X is any amino acid residue. |
| Claim: |
2. The matrix metalloproteinase inhibitor and down-regulator according to claim 1 wherein the peptide motif is CRVYGPYLLC (SEQ ID NO: 7). |
| Claim: |
3. A pharmaceutical composition comprising a matrix metalloproteinase inhibitor and down-regulator according to claim 1 and a pharmaceutically acceptable carrier. |
| Claim: |
4. The use of a matrix metalloproteinase inhibitor and down-regulator according to claim 1 for the manufacture of a pharmaceutical composition for the treatment of matrix metalloproteinase (MMP) dependent conditions. |
| Claim: |
5. The use according to claim 4 for the manufacture of a pharmaceutical composition for the treatment of conditions dependent on MMP-2 and/or MMP-9. |
| Claim: |
6. A process for the preparation of a matrix metalloproteinase inhibitor/down-regulator according to claim 1, which process comprises solid-phase Merrifield peptide synthesis. |
| Claim: |
7. A method for the therapeutic or prophylactic treatment of matrix metalloproteinase dependent conditions in mammals comprising administering to said mammal a matrix metalloproteinase inhibitor/down-regulator according to claim 1 in an amount which is effective in inhibiting and down-regulating MMP activations, expressions and/or functions in said mammal. |
| Claim: |
8. The method according to claim 7 for the therapeutic or prophylactic treatment of conditions dependent on MMP-2 and/or MMP-9. |
| Claim: |
9. A method for inhibiting the activations, expressions, functions and actions of matrix metalloproteinases in mammals, comprising administering to said mammal a matrix metalloproteinase inhibitor and down-regulator according to claim 1 in an amount which is effective in blocking the activities, activations and actions of MMPs. |
| Claim: |
10. The method according to claim 9 for inhibiting the expressions, activations and actions of MMP-2 and/or MMP-9. |
| Claim: |
11. A method for inhibiting and down-regulating matrix metalloproteinases in vitro comprising adding to an in vitro system a matrix metalloproteinase inhibitor and down-regulator according to claim 1 in an amount which is effective in inhibiting and down-regulating the MMP activity. |
| Claim: |
12. The method according to claim 11 wherein the matrix metalloproteinases to be inhibited and down-regulated are MMP-2 and/or MMP-9. |
| Claim: |
13. The use of a matrix metalloproteinase inhibitor and down-regulator according to claim 1 in biochemical isolation and purification procedures of matrix metalloproteinases. |
| Claim: |
14. Use of matrix metalloproteinase inhibitor and down-regulator according to claim 1 in improving targeting of liposomes to tumor cells. |
| Claim: |
15. Use according to claim 14, wherein the tumor cells are tumor cells expressing matrix metalloproteinases. |
| Current U.S. Class: |
514015/000 |
| Current International Class: |
61; 07 |
| رقم الانضمام: |
edspap.20070207967 |
| قاعدة البيانات: |
USPTO Patent Applications |