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• W3136176846 startingPage "215" @default.
• W3136176846 abstract "The P2X receptor 7 (P2X7R) is a plasma membrane receptor sensing extracellular ATP associated with a wide variety of cellular functions. It is most commonly expressed on immune cells and is highly upregulated in a number of human cancers where it can play a trophic role in tumorigenesis. Activation of this receptor leads to the formation of a non-selective cation channel, which has been associated with several cellular functions mediated by the PI3K/Akt pathway and protein kinases. Due to its broad range of functions, the receptor represents a potential therapeutic target for a number of cancers. This review describes the range of mechanisms associated with P2X7R activation in cancer settings and highlights the potential of targeted inhibition of P2X7R as a therapy. It also describes in detail a number of key P2X7R antagonists currently in pre-clinical and clinical development, including oxidised ATP, Brilliant Blue G (BBG), KN-62, KN-04, A740003, A438079, GSK1482160, CE-224535, JNJ-54175446, JNJ-55308942, and AZ10606120. Lastly, it summarises the in vivo studies and clinical trials associated with the use and development of these P2X7R antagonists in different disease contexts." @default.
• W3136176846 created "2021-03-29" @default.
• W3136176846 creator A5015997735 @default.
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• W3136176846 creator A5079459105 @default.
• W3136176846 date "2021-03-17" @default.
• W3136176846 modified "2023-10-17" @default.
• W3136176846 title "Antagonism of the ATP-gated P2X7 receptor: a potential therapeutic strategy for cancer" @default.
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