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Changxiu Qu

As seen in: Science Magazine
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Articles

Ligand recognition, unconventional activation, and G protein coupling of the prostaglandin E2 receptor EP2 subtype

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By Changxiu Qu, Chunyou Mao, Peng Xiao, Qingya Shen
| Science Magazine Verified
Abstract Selective modulation of the heterotrimeric G protein α S subunit–coupled prostaglandin E2 (PGE2) receptor EP2 subtype is a promising therapeutic strategy for osteoporosis, ocular hypertension, neurodegenerative diseases, and cardiovascular disorders. Here, we report the cryo–electron microscopy structure of the EP2-Gs complex with its endogenous agonist PGE2 and two synthesized agonists, taprenepag and evatanepag (CP-533536).
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Ligand recognition and allosteric regulation of DRD1-Gs signaling complexes

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By Peng Xiao, Wei Yan, Lu Gou, Liangliang Kong, Chao Wu, Xin Wen, Yuan Yuan, Sheng Cao, Xin Yang, Anjie Xia, Qianqian Zhang, Chao Zhang, Gui-Hua Hou, Ya-Ni Zhong, Changxiu Qu, Chuan-Cheng Yang, Zhenquan Hu, Yong-Hao He, Dao-Lai Zhang, Huanxiang Liu, Lizhe Zh
| ScienceDirect Verified
Highlights • Structures of DRD1-Gs in complex with catechol-based and non-catechol agonists • Key polar interaction network is involved in DRD1 activation • Specific features for agonists interaction and Gs coupling of DRD1 are determined • Structure of DRD1-Gs complexed with dopamine and positive allosteric modulator • Structural basis of allosteric regulation of DRD1 by LY3154207 is investigated Summary Dopamine receptors, including D1- and D2-like receptors, are important therapeutic...
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