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LETTERS TO THE EDITOR

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

Youwei Xu^1,†,* , Hongmin Cai^1,† , Chongzhao You^1,2 , Xinheng He^1,2 , Qingning Yuan¹ , Hualiang Jiang^1,2,3,4 , Xi Cheng^1,4 , Yi Jiang¹ , H. Eric Xu^1,2,3,*

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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