Key result
P2Y6R antagonists, such as MRS2578, represent a promising therapeutic strategy for inflammatory diseases by targeting the PLC pathway and intracellular calcium release.
Why the study?
P2Y6R plays a physiological role in mediating inflammation, suggesting it could be a promising molecular target for treating inflammatory diseases, with several antagonists discovered over the past ten years.
P2Y6R antagonists, such as MRS2578, represent a promising molecular target and therapeutic strategy for the treatment of inflammatory diseases.
P2Y6R may support targeted anti-inflammatory therapy; leaves open clinical validation in dedicated trials.
P2Y receptors (P2YRs) are G protein-coupled receptors that are activated by extracellular nucleotides. The P2Y6 receptor (P2Y6R) is specifically activated by UDP, causing PKC activation and intracellular calcium ion release through the PLC pathway. Based on receptor tissue distribution and related pathways, several studies have reported that P2Y6R plays a physiological role in mediating inflammation, which suggests that P2Y6R could be a promising molecular target for the treatment of inflammatory diseases. In the past ten years, several P2Y6R antagonists have been discovered as new therapeutic strategies for inflammatory diseases. In this article, we systematically summarize the role of P2Y6R in inflammation and highlight the anti-inflammatory mechanism of a key P2Y6R antagonist, MRS2578. Insight into recent progress on the discovery of P2Y6R antagonists is also discussed.
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Wang et al. (2022) conducted a review in Inflammatory diseases. P2Y6R antagonists (e.g., MRS2578) was evaluated. P2Y6R antagonists, such as MRS2578, represent a promising therapeutic strategy for inflammatory diseases by targeting the PLC pathway and intracellular calcium release.
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