The non-competitive metabotropic glutamate receptor-1 antagonist CPCCOEt inhibits the in vitro growth of human melanoma

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 sti...

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Veröffentlicht in:Oncology reports 2007-06, Vol.17 (6), p.1399-1404
Hauptverfasser: HAAS, Helga Susanne, PFRAGNER, Roswitha, SIEGL, Veronika, INGOLIC, Elisabeth, HEINTZ, Elfgard, SCHRAML, Elisabeth, SCHAUENSTEIN, Konrad
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container_end_page 1404
container_issue 6
container_start_page 1399
container_title Oncology reports
container_volume 17
creator HAAS, Helga Susanne
PFRAGNER, Roswitha
SIEGL, Veronika
INGOLIC, Elisabeth
HEINTZ, Elfgard
SCHRAML, Elisabeth
SCHAUENSTEIN, Konrad
description 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.
doi_str_mv 10.3892/or.17.6.1399
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subjects Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Proliferation - drug effects
Chromones - pharmacology
Dermatology
Drug Resistance, Neoplasm - drug effects
Excitatory Amino Acid Antagonists - pharmacology
Glutamic Acid - metabolism
Humans
Medical sciences
Melanoma - metabolism
Melanoma - ultrastructure
Receptors, Metabotropic Glutamate - antagonists & inhibitors
Skin Neoplasms - metabolism
Skin Neoplasms - ultrastructure
Taxoids - pharmacology
Tumor Cells, Cultured
Tumors
Tumors of the skin and soft tissue. Premalignant lesions
title The non-competitive metabotropic glutamate receptor-1 antagonist CPCCOEt inhibits the in vitro growth of human melanoma
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