The potential of P2X7 receptors as a therapeutic target, including inflammation and tumour progression.

The potential of P2X7 receptors as a therapeutic target, including inflammation and tumour progression.
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DOI:
10.1007/s11302-017-9593-0
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发表时间:
2018-03
影响因子:
3.5
通讯作者:
Knight GE
Knight GE
中科院分区:
医学3区
文献类型:
--
作者:
Burnstock G;Knight GE

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七个P2X离子通道核苷酸受体亚型已被克隆和表征。P2X7受体(P2X7R)是不寻常的,因为在细胞内C端有额外的氨基酸。低浓度的ATP有时会打开阳离子通道,导致细胞增殖,而高浓度的ATP会打开大孔隙,释放炎症细胞因子,导致细胞凋亡。由于许多疾病涉及炎症和免疫反应,而P2X7R调节炎症,最近人们对P2X7R的病理生理作用和P2X7R拮抗剂治疗多种疾病的潜力感兴趣。这些疾病包括神经退行性疾病、精神疾病、癫痫和一些外周器官疾病,包括心血管、呼吸道、肾脏、肝脏、膀胱、皮肤和肌肉骨骼。讨论了P2X7R药物治疗肿瘤进展的潜力。
Seven P2X ion channel nucleotide receptor subtypes have been cloned and characterised. P2X7 receptors (P2X7R) are unusual in that there are extra amino acids in the intracellular C terminus. Low concentrations of ATP open cation channels sometimes leading to cell proliferation, whereas high concentrations of ATP open large pores that release inflammatory cytokines and can lead to apoptotic cell death. Since many diseases involve inflammation and immune responses, and the P2X7R regulates inflammation, there has been recent interest in the pathophysiological roles of P2X7R and the potential of P2X7R antagonists to treat a variety of diseases. These include neurodegenerative diseases, psychiatric disorders, epilepsy and a number of diseases of peripheral organs, including the cardiovascular, airways, kidney, liver, bladder, skin and musculoskeletal. The potential of P2X7R drugs to treat tumour progression is discussed.
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