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Structure paper

TitleMolecular basis of antagonism of the dimeric human arginine vasopressin receptor 1A.
Journal, issue, pagesNat Commun, Year 2026
Publish dateJan 16, 2026
AuthorsPeiyu Zhong / Bingxin Chu / Zijing Yu / Yu Qiao / Yu Ding / Yongdeng Zhang / Xudong Wu /
PubMed AbstractArginine vasopressin (AVP) and oxytocin (OT) are peptide hormones critical for various physiological processes. Vasopressin receptor 1 A (V1aR), a primary AVP target, is promising for central ...Arginine vasopressin (AVP) and oxytocin (OT) are peptide hormones critical for various physiological processes. Vasopressin receptor 1 A (V1aR), a primary AVP target, is promising for central nervous system (CNS) disorders therapies, yet the mechanisms of antagonism and oligomerization remain poorly understood. Here, we present structures of human V1aR in its apo state and in complexes with antagonists: atosiban, balovaptan, and SRX246. Structural analyses reveal a dimeric V1aR assembly, validated by functional assays and imaging in cells. The apo structure shows a flat extracellular loop 2 (ECL2) with unpaired cysteines, undergoing significant conformational changes upon ligand binding. Antagonist-bound structures, combined with mutagenesis and radioligand binding assays, uncover distinct binding modes and key determinants for antagonism and selectivity. These findings provide a comprehensive understanding of V1aR assembly and dynamic regulation, offering valuable insights for structure-guided development of new antagonists targeting dimeric V1aR for CNS disorders.
External linksNat Commun / PubMed:41545407
MethodsEM (single particle)
Resolution2.8 Å
Structure data

64555

9uwi

EMDB-64555, PDB-9uwi:
Cryo-EM structure of human V1aR bound with atosiban at a resolution of 2.8 angstrom
Method: EM (single particle) / Resolution: 2.8 Å

Chemicals

ChemComp-CLR:
CHOLESTEROL

Source
  • homo sapiens (human)
  • synthetic construct (others)
KeywordsSIGNALING PROTEIN / GPCR / small molecule / antagonist / nanobody

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