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Molecular basis of lipid and ligand regulation of prostaglandin receptor DP2

Proc Natl Acad Sci U S A .. 2024-12; 
Jiuyin Xu , Youwei Xu , Li Hou , Xinheng He , Yang Li , Jing Zhao , Xue Meng , James Jiqi Wang , Yanli Wu , Heng Zhang , Yunhai Li , Wen Hu , Qingning Yuan , Kai Wu , Xi Cheng , Yi Jiang , Yu Xia , H Eric Xu , Canrong Wu
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Abstract

Prostaglandin D2 receptor 2 (DP2) is an important anti-inflammatory and antiallergic drug target. While inactive DP2 structures are known, its activation mechanisms and biased signaling remain unclear. Here, we report cryo-EM structures of an apo DP2-Gi complex, a DP2-Gi complex bound to the endogenous ligand Prostaglandin D2 (PGD2), and a DP2-Gi complex bound to indomethacin, an arrestin-biased ligand, at resolutions of 2.5 Å, 2.8Å, and 2.3 Å, respectively. These structures reveal a distinct binding pose of PGD2 and indomethacin and provide key insights into receptor activation and transducer coupling. Combining the structural data with functional studies, we uncover the molecular basis for biased signaling... More

Keywords

DP2; lipid regulation; prostaglandin receptor; receptor activation; signal bias.