Reference - Detail
| RRC ID | 61207 |
|---|---|
| Author | Shinoda K, Shibuya M, Hibino S, Ono Y, Matsuda K, Takemura A, Zou D, Kokubo Y, Takechi A, Kudoh S. |
| Title | A novel matrix metalloproteinase inhibitor, FYK-1388 suppresses tumor growth, metastasis and angiogenesis by human fibrosarcoma cell line. |
| Journal | Int J Oncol |
| Abstract |
The matrix metalloproteinases (MMPs) are likely to contribute to tumor cell invasion, metastasis and angiogenesis. Several MMP inhibitors have been developed, recently and their anti-tumor efficacy is being evaluated in clinical trials. FYK-1388 is a novel broad MMP inhibitor which blocks the activity of MMP-1, -2, -3, -7, -9, -13 and -14 (MT-MMP-1). It is especially effective against MMP-2 and -9 more so than other MMP inhibitors such as Marimastat, Ro 32-3555 and D-2163. Here, we investigated the anti-tumor efficacy of FYK-1388 using the human fibrosarcoma cell line HT-1080. These cells produced MMP-2 and -9, which FYK-1388 inhibited at a dose of 10(-8) M. FYK-1388 at 0.2 mg/mouse/day significantly suppressed tumor growth when given by s.c. injection for 22 days, experimental lung metastasis after 5 days s.c. injection and also suppressed tumor-induced angiogenesis in the dorsal air sac assay after 7 days s.c. injection. In the MTT assay, FYK-1388 had no effect on the in vitro growth of HT-1080 cells. These results suggest that FYK-1388 possesses anti-tumor efficacy as a result of inhibiting angiogenesis through the suppression of MMP-2 and -9 activity. |
| Volume | 22(2) |
| Pages | 281-8 |
| Published | 2003-2-1 |
| PMID | 12527923 |
| MeSH | Angiogenesis Inhibitors / pharmacology Angiogenesis Inhibitors / therapeutic use* Animals Antineoplastic Agents / pharmacology Antineoplastic Agents / therapeutic use* Female Fibrosarcoma / blood supply Fibrosarcoma / drug therapy* Fibrosarcoma / enzymology Fibrosarcoma / pathology Fibrosarcoma / prevention & control Fibrosarcoma / secondary Guanidines / chemistry Guanidines / pharmacology Guanidines / therapeutic use* Humans Hydroxamic Acids / chemistry Hydroxamic Acids / pharmacology Hydroxamic Acids / therapeutic use* Injections, Subcutaneous Lung Neoplasms / prevention & control Lung Neoplasms / secondary Matrix Metalloproteinase Inhibitors* Mice Mice, Inbred BALB C Mice, Inbred ICR Mice, Nude Molecular Structure Neoplasm Proteins / antagonists & inhibitors* Protease Inhibitors / pharmacology Protease Inhibitors / therapeutic use* Tumor Cells, Cultured / drug effects Xenograft Model Antitumor Assays |
| IF | 3.899 |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | Patent(IFI CLAIMS) |
| Total number of mentions | 14 |
| Altmetric score changes over past 6months | 3.0 |
| Resource | |
| Human and Animal Cells | NB1RGB(RCB0222) |