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TitleStructural insight into ligand binding and activation of the orphan GPCR Mas1.
Journal, issue, pagesEMBO J, Year 2026
Publish dateMar 30, 2026
AuthorsYumu Zhang / Qiuying Wang / Heng Liu / Hong Shan / Yimin Gu / Jiaqi Yang / Yuan Gao / Kai Wu / Dehua Yang / H Eric Xu /
PubMed AbstractThe Mas1 receptor, an orphan class A G-protein-coupled receptor (GPCR), plays pivotal roles in cardiovascular and anti-inflammatory regulation. Despite its therapeutic relevance, the structural ...The Mas1 receptor, an orphan class A G-protein-coupled receptor (GPCR), plays pivotal roles in cardiovascular and anti-inflammatory regulation. Despite its therapeutic relevance, the structural mechanisms underlying Mas1 ligand binding and activation remain poorly understood. Here, we report cryo-EM structures of Mas1 bound to two chemically distinct agonists-neuropeptide FF (NPFF) and synthetic small-molecule AR234958-captured in complex with inhibitory G proteins. These structures reveal a conserved orthosteric binding pocket accommodating both ligands through shared hydrophobic interactions. Unlike many other class A GPCRs that rely on direct W toggle switch engagement, Mas1 adopts a non-canonical activation strategy driven by a ligand-induced hydrophobic compression plane involving residues Y248, L87, I84, and L266 at the bottom of the ligand binding pocket. This mechanism transmits mechanical tension to promote TM6 displacement and G protein coupling. Functional mutagenesis validates this model, identifying two transmembrane helix 6 (TM6) residues, M244 and F237, as critical molecular switches. Comparative analyses of Mas1-related receptors, MRGPRX1-X4, reveal conserved features and mechanistic divergence within this subfamily. These findings provide a structural framework for understanding Mas1 pharmacology and rational design of selective therapeutics.
External linksEMBO J / PubMed:41912627
MethodsEM (single particle)
Resolution2.54 - 2.77 Å
Structure data

66514

9x3y

EMDB-66514, PDB-9x3y:
NPFF bound Mas1 Receptor
Method: EM (single particle) / Resolution: 2.77 Å

66515

9x3z

EMDB-66515, PDB-9x3z:
NPFF bound Mas1 Receptor Complex
Method: EM (single particle) / Resolution: 2.54 Å

Source
  • homo sapiens (human)
KeywordsPEPTIDE BINDING PROTEIN / GPCR / Agonist / Orphan Receptor

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