G-protein-coupled receptors (GPCRs) represent a class of therapeutic targets that have been widely exploited for drug designs and development. Metabotropic glutamate receptors (mGluRs) belong to Class C GPCRs and are predominantly involved in maintaining cellular homeostasis in the central nervous system (CNS). The surprising accumulating evidence suggesting other functional roles of mGluRs in human malignancies in addition to synaptic transmission has presented intriguing possibilities to make mGluRs putative novel targets for human cancers. Since our group first described the aberrant expression of mGluR1 as the driving force in melanomagenesis in transgenic mouse models, other subtypes of mGluRs have been implicated in the pathogenesis of various cancer types such as malignant gliomas and medulloblastomas. As such, increased efforts have been generated to elucidate the mechanisms by which mGluRs confer oncogenic potential. Current knowledge on the participation of various mGluRs in several human cancers suggests that mGluRs are ‘druggable’ members of the GPCR superfamily and their oncogenic implications in cancer, so further understanding on anti-mGluR strategies will be beneficial.WIREs Membr Transp Signal 2012, 1:211–220. doi: 10.1002/wmts.21
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