Abstract | PURPOSE: We examined the anti- tumor effect of 5-S-GAD, a novel potent inhibitor of protein tyrosine kinases, isolated from the flesh fly in order to investigate the potential use of this compound as an anti- tumor agent. METHODS: In vitro growth inhibition was evaluated using the alamarBlue assay kit. In vivo anti- tumor activity was evaluated by i.p. treatment of 5-S-GAD against xenografted melanoma (LOX-IMV1) and breast carcinoma (MDA-MB-435S) in nude mice. RESULTS: Of 38 human cancer cell lines examined, this compound showed significant cytotoxicity toward two estrogen-negative breast carcinomas (MDA-MB-231 and MDA-MB-435S) and one malignant melanoma (LOX-IMV1) in vitro, indicating that it exhibits selective cytotoxicity to certain tumor cell lines. In accordance with its in vitro anti- tumor effect, 5-S-GAD was shown to significantly repress the growth of sensitive tumor cells in nude mice. CONCLUSION: These results indicate that 5-S-GAD is potentially useful to treat certain human cancer.
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Authors | N Akiyama, M Hijikata, A Kobayashi, T Yamori, T Tsuruo, S Natori |
Journal | Anticancer research
(Anticancer Res)
2000 Jan-Feb
Vol. 20
Issue 1A
Pg. 357-62
ISSN: 0250-7005 [Print] Greece |
PMID | 10769680
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Benzoquinones
- Enzyme Inhibitors
- Lactams, Macrocyclic
- N-beta-alanyl-5-S-glutathionyl-3,4-dihydroxyphenylalanine
- Neoplasm Proteins
- Quinones
- Rifabutin
- Dihydroxyphenylalanine
- herbimycin
- Protein-Tyrosine Kinases
- Glutathione
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Topics |
- Animals
- Antineoplastic Agents
(pharmacology, therapeutic use)
- Benzoquinones
- Breast Neoplasms
(pathology)
- Dihydroxyphenylalanine
(analogs & derivatives, pharmacology, therapeutic use)
- Diptera
(chemistry)
- Drug Screening Assays, Antitumor
- Enzyme Inhibitors
(pharmacology, therapeutic use)
- Female
- Glutathione
(analogs & derivatives, pharmacology, therapeutic use)
- Humans
- Lactams, Macrocyclic
- Mammary Neoplasms, Experimental
(drug therapy)
- Melanoma
(pathology)
- Melanoma, Experimental
(drug therapy)
- Mice
- Mice, Nude
- Molecular Structure
- Neoplasm Proteins
(antagonists & inhibitors)
- Neoplasm Transplantation
- Protein-Tyrosine Kinases
(antagonists & inhibitors)
- Quinones
(pharmacology)
- Rifabutin
(analogs & derivatives)
- Transplantation, Heterologous
- Tumor Cells, Cultured
(drug effects, transplantation)
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