mGlu Receptors and Cancerous Growth.
mGlu Receptors and Cancerous Growth.
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DOI：
10.1002/wmts.21
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发表时间：
2012-03
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G蛋白偶联受体（GPCR）是一类治疗靶点，已在药物设计和开发中得到广泛应用。代谢型谷氨酸受体（mGluRs）属于C类GPCR，主要参与维持中枢神经系统（CNS）的细胞内稳态。越来越多令人惊讶的证据表明，mGluRs除了在突触传递中起作用外，在人类恶性肿瘤中还具有其他功能，这为将mGluRs作为人类癌症的新型潜在靶点提供了有趣的可能性。自从我们的研究小组首次在转基因小鼠模型中描述mGluR1的异常表达是黑色素瘤发生的驱动因素以来，mGluRs的其他亚型也被认为与多种癌症类型的发病机制有关，例如恶性胶质瘤和髓母细胞瘤。因此，人们加大了努力来阐明mGluRs赋予致癌潜能的机制。目前关于多种mGluRs参与几种人类癌症的知识表明，mGluRs是GPCR超家族中“可成药的”成员，并且它们在癌症中具有致癌作用，因此进一步了解抗mGluR策略将是有益的。
G-protein coupled receptors (GPCR) 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 potentials. 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.