Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Haas, HS; Pfragner, R; Siegl, V; Ingolic, E; Heintz, E; Schraml, E; Schauenstein, K.
The non-competitive metabotropic glutamate receptor-1 antagonist CPCCOEt inhibits the in vitro growth of human melanoma.
Oncol Rep. 2007; 17(6): 1399-1404.
Doi: 10.3892/or.17.6.1399
Web of Science
PubMed
FullText
FullText_MUG
- Führende Autor*innen der Med Uni Graz
- Haas Helga Susanne
- Co-Autor*innen der Med Uni Graz
- Pfragner Roswitha
- Schraml Elisabeth
- Siegl Veronika
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- Abstract:
- Five decades ago, the dicarboxylic amino acid glutamate became recognized as the major excitatory neurotransmitter in the central nervous system. In recent years, the expression of glutamate receptors was detected also in peripheral, non-neuronal tissues. Furthermore, it was found that glutamate stimulated the proliferation and migration of several peripheral tumor cells, and that glutamate receptor antagonists limited tumor growth. Most of these studies, however, used broad spectrum compounds and/or group-specific antagonists. Here we report that a selective, non-competitive metabotropic glutamate receptor-1 antagonist, CPCCOEt (7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester), significantly inhibited the proliferation and modified the morphology of two human melanoma cell lines. These effects were independent of the external glutamate level in the culture medium. In addition, CPCCOEt significantly enhanced the tumoricidal effects of cytostatic drugs. Thus, selective non-competitive metabotropic glutamate receptor antagonists may be used alone and/or with the synergistic effects of chemotherapy, thus enhancing existing therapies of melanoma and possibly other malignancies.
- Find related publications in this database (using NLM MeSH Indexing)
- Antineoplastic Agents - pharmacology
- Cell Proliferation - drug effects
- Chromones - pharmacology
- Drug Resistance, Neoplasm - drug effects
- Excitatory Amino Acid Antagonists - pharmacology
- Glutamic Acid - metabolism
- Humans - metabolism
- Melanoma - metabolism
- Receptors, Metabotropic Glutamate - antagonists and inhibitors
- Skin Neoplasms - metabolism
- Taxoids - pharmacology
- Tumor Cells, Cultured - pharmacology
- Find related publications in this database (Keywords)
- metabotropic glutamate receptors
- non-competitive metabotropic glutamate receptor antagonist
- human melanoma
- cell proliferation
- tumor growth