Purinergic Signal. 2013 Dec;9(4):491-540. doi: 10.1007/s11302-013-9372-5.
Receptors for extracellular nucleotides are widely expressed by mammalian cells. They mediate a large array of responses ranging from growth stimulation to apoptosis, from chemotaxis to cell differentiation and from nociception to cytokine release, as well as neurotransmission. Pharma industry is involved in the development and clinical testing of drugs selectively targeting the different P1 nucleoside and P2 nucleotide receptor subtypes. As described in detail in the present review, P2 receptors are expressed by all tumours, in some cases to a very high level. Activation or inhibition of selected P2 receptor subtypes brings about cancer cell death or growth inhibition. The field has been largely neglected by current research in oncology, yet the evidence presented in this review, most of which is based on in vitro studies, although with a limited amount from in vivo experiments and human studies, warrants further efforts to explore the therapeutic potential of purinoceptor targeting in cancer.
细胞外核苷酸的受体广泛存在于哺乳动物细胞中。它们介导了一系列广泛的反应,从生长刺激到细胞凋亡,从趋化作用到细胞分化,从痛觉到细胞因子释放,以及神经传递。制药行业正在开发和临床测试选择性针对不同 P1 核苷和 P2 核苷酸受体亚型的药物。正如本综述中详细描述的那样,P2 受体存在于所有肿瘤中,在某些情况下表达水平非常高。激活或抑制选定的 P2 受体亚型会导致癌细胞死亡或生长抑制。这个领域在肿瘤学的当前研究中被忽视了,但本综述中提出的证据,其中大部分基于体外研究,尽管从体内实验和人体研究中获得的证据有限,但值得进一步努力探索嘌呤受体靶向在癌症治疗中的潜力。