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LETTERS TO THE EDITOR

Structural insights into ligand binding and activation of the human thyrotropin-releasing hormone receptor

Youwei Xu1,†,* , Hongmin Cai1,† , Chongzhao You1,2 , Xinheng He1,2 , Qingning Yuan1 , Hualiang Jiang1,2,3,4 , Xi Cheng1,4 , Yi Jiang1 , H. Eric Xu1,2,3,*

1The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
2University of Chinese Academy of Sciences, Beijing, China
3School of Life Science and Technology, ShanghaiTech University, Shanghai, China
4State Key Laboratory of Drug Research and CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
These authors contributed equally: Youwei Xu, Hongmin Cai
* Correspondence: Youwei Xu(xuyouwei@simm.ac.cn)H. Eric Xu(eric.xu@simm.ac.cn)

Dear Editor,

The thyrotropin-releasing hormone (TRH) is the initial hormone of the hypothalamo–pituitary–thyroid axis (HPT), a signaling cascade required for metabolic homeostasis and development in vertebrates. TRH is a tripeptide hormone (pGlu–His–Pro-NH2) that is synthesized in the hypothalamus and activates thyrotropin-releasing hormone receptor (TRHR), a member of class A G protein-coupled receptor (GPCR). Activated TRHR couples to Gq and activates the phosphatidylinositol (IP3)-calcium-protein kinase C (PKC) pathway1 that ultimately leads to upregulation of thyroid hormones.


https://doi.org/10.1038/s41422-022-00641-x

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