Potential therapeutic targets for ATP-gated P2X receptor ion channels.
P2X receptors make up a novel family of ligand-gated ion channels that are activated by binding of extracellular ATP. These receptors can form a number of homomeric and heteromeric ion channels, which are widely distributed throughout the human body. They are thought to play an important role in many cellular processes, including synaptic transmission and thrombocyte aggregation. These ion channels are also involved in the pathology of several disease states, including chronic inflammation and neuropathic pain, and thus are the potential targets for drug development. The recent discovery of potent and highly selective antagonists for P2X(7) receptors, through the use of high-throughput screening, has helped to further understand the P2X receptor pharmacology and provided new evidence that P2X(7) receptors play a specific role in chronic pain states. In this review, we discuss how the P2X family of ion channels has distinguished itself as a potential new drug target. We are optimistic that safe and effective candidate drugs will be suitable for progression into clinical development.
Li
Zhiyuan
Z
Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, People's Republic of China. liz@slu.edu
Liang
Dong
D
Chen
Ling
L
D000255:Adenosine Triphosphate / Q000502:physiology*; D001665:Binding Sites; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects*; D008024:Ligands; D010146:Pain / Q000188:drug therapy; D058910:Purinergic P2 Receptor Agonists; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2 / Q000187:drug effects*; D058469:Receptors, Purinergic P2X; D013927:Thrombosis / Q000188:drug therapy; D014570:Urologic Diseases / Q000188:drug therapy
D008024:Ligands; D058910:Purinergic P2 Receptor Agonists; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058469:Receptors, Purinergic P2X; D000255:Adenosine Triphosphate