mGlu Receptors and Cancerous Growth.

Jessica Teh, Suzie Chen
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引用次数: 30

Abstract

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.

mGlu受体与癌变生长
g蛋白偶联受体(GPCR)是一类广泛用于药物设计和开发的治疗靶点。代谢性谷氨酸受体(mGluRs)属于C类gpcr,主要参与维持中枢神经系统(CNS)的细胞稳态。越来越多令人惊讶的证据表明,除了突触传递外,mGluRs在人类恶性肿瘤中还具有其他功能作用,这为mGluRs被认为是人类癌症的新靶点提供了有趣的可能性。由于我们的研究小组首次在转基因小鼠模型中描述了mGluR1的异常表达是黑色素瘤形成的驱动力,因此mGluR1的其他亚型与各种癌症类型(如恶性胶质瘤和成神经管细胞瘤)的发病机制有关。因此,越来越多的人致力于阐明mGluRs赋予致癌潜力的机制。目前关于各种mglur参与几种人类癌症的知识表明,mglur是GPCR超家族的“可药物”成员及其在癌症中的致癌作用,因此进一步了解抗mglur策略将是有益的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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