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TitleCryo-EM structures of GnRHR: Foundations for next-generation therapeutics.
Journal, issue, pagesProc Natl Acad Sci U S A, Vol. 122, Issue 25, Page e2500112122, Year 2025
Publish dateJun 24, 2025
AuthorsShiyi Shen / Xinheng He / Heng Liu / Wen Hu / H Eric Xu / Jia Duan /
PubMed AbstractGonadotropin-releasing hormone receptor (GnRHR) is critical for reproductive health and a key therapeutic target for endocrine disorders and hormone-responsive cancers. Using high-resolution ...Gonadotropin-releasing hormone receptor (GnRHR) is critical for reproductive health and a key therapeutic target for endocrine disorders and hormone-responsive cancers. Using high-resolution cryoelectron microscopy, we determined the structures of and GnRHRs bound to mammal GnRH, uncovering conserved and species-specific mechanisms of receptor activation and G protein coupling. The conserved "U"-shaped GnRH conformation mediates high-affinity binding through key interactions with residues such as K, Y, and Y. Species-specific variations in extracellular loops and receptor-ligand contacts fine-tune receptor function, while ligand binding induces structural rearrangements, including N terminus displacement and TM6 rotation, critical for signaling. Structure-activity relationship analysis demonstrates how D-amino acid substitutions in GnRH analogs enhance stability and receptor affinity. Distinct binding modes of agonists and antagonists elucidate mechanisms of ligand-dependent activation and inactivation. These insights lay the groundwork for designing next-generation GnRHR therapeutics with enhanced specificity and efficacy for conditions like endometriosis, prostate cancer, and infertility.
External linksProc Natl Acad Sci U S A / PubMed:40523184 / PubMed Central
MethodsEM (single particle)
Resolution2.67 - 3.18 Å
Structure data

63857

9u4w

EMDB-63857, PDB-9u4w:
cryo-EM structure of pig GnRHR bound with mammal GnRH
Method: EM (single particle) / Resolution: 3.18 Å

63858

9u4y

EMDB-63858, PDB-9u4y:
cryo-EM structure of Xenopus laevis GnRHR bound with mammal GnRH
Method: EM (single particle) / Resolution: 2.67 Å

Source
  • sus scrofa (pig)
  • homo sapiens (human)
  • xenopus laevis (African clawed frog)
  • synthetic construct (others)
  • ateles (mammal)
KeywordsMEMBRANE PROTEIN / Cryo-EM / gonadotropin releasing hormone receptor / GnRHR / Gonadotropin-Releasing Hormone Receptor

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