Title:P2Y6R: A Promising New Target in Inflammatory Diseases and Advances in its Antagonists
Volume: 30
Issue: 19
Author(s): Yuanhui Wang, Yuanyuan Pei, Yongfang Yao, Weyland Cheng, Yinchao Li*Yongtao Duan*
Affiliation:
- School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, China
- Henan Provincial Key Laboratory of Children's Genetics and Metabolic Diseases, Children's Hospital Affiliated to Zhengzhou University, Zhengzhou University, Zhengzhou 450018, China
Keywords:
P2Y6R, inflammation, antagonist, mechanism, nucleotides, therapeutic strategies.
Abstract: 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.