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TitleDecoding the structural basis of ligand recognition and biased signaling in the motilin receptor.
Journal, issue, pagesCell Rep, Vol. 44, Issue 3, Page 115329, Year 2025
Publish dateMar 25, 2025
AuthorsChongzhao You / Mengting Jiang / Tianyu Gao / Zining Zhu / Xinheng He / Youwei Xu / Yuan Gao / Yi Jiang / H Eric Xu /
PubMed AbstractThe motilin receptor (MTLR) is a key target for treating gastrointestinal (GI) disorders like gastroparesis, yet developing effective agonists remains challenging due to drug tolerance and signaling ...The motilin receptor (MTLR) is a key target for treating gastrointestinal (GI) disorders like gastroparesis, yet developing effective agonists remains challenging due to drug tolerance and signaling bias. We present cryoelectron microscopy (cryo-EM) structures of MTLR bound to azithromycin, a macrolide antibiotic, and DS-3801b, a non-macrolide agonist. Distinct ligand recognition mechanisms are revealed, with azithromycin binding deeply within the orthosteric pocket and DS-3801b adopting a special clamp-like conformation stabilized by a water molecule. We also highlight the critical role of extracellular loop 2 (ECL2) in ligand specificity and signaling pathway activation, affecting both G-protein and β-arrestin signaling. Additionally, the "DRS" motif and interactions around transmembranes 6/7 (TM6/7) are identified as key drivers of signaling selectivity. These findings offer insights into the structural dynamics of MTLR, laying the groundwork for the rational design of next-generation GI prokinetic drugs with enhanced efficacy and safety.
External linksCell Rep / PubMed:39987561
MethodsEM (single particle)
Resolution2.57 - 2.74 Å
Structure data

61597

9jmc

EMDB-61597, PDB-9jmc:
Cryo-EM structure of the DS-3801b-Motilin receptor-Gq protein complex
Method: EM (single particle) / Resolution: 2.57 Å

61598

9jmd

EMDB-61598, PDB-9jmd:
Cryo-EM structure of the Azithromycin-Motilin receptor-Gq protein complex
Method: EM (single particle) / Resolution: 2.74 Å

Chemicals

ChemComp-CLR:
CHOLESTEROL

PDB-1l4h:
Crystal Structure of CobT complexed with indole and nicotinate mononucleotide

ChemComp-HOH:
WATER

ChemComp-ZIT:
AZITHROMYCIN / antibiotic*YM

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsSIGNALING PROTEIN / Cryo-EM / GPCR / Motilin receptor / DS-3801b / macrolide antibiotics / Gq / complex / Azithromycin

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