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Structural basis for motilin and erythromycin recognition by motilin receptor

Science Advances. 2023-03; 
Chongzhao You, Yumu Zhang, Youwei Xu, Peiyu Xu, Zhen Li, Huadong Li, Sijie Huang, Zecai Chen, Jingru Li, H Eric Xu, Yi Jiang
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Peptide Synthesis Cell pellets were thawed in 20 mM Hepes (pH 7.4), 50 mM NaCl, 10 mM MgCl2, and CaCl2 supplemented with Protease Inhibitor Cocktail (TargetMol). For the motilin-MTLR-Gq-scFv16 complex, 15 μM motilin (GenScript) and apyrase (25 mU ml−1 Get A Quote

Abstract

Motilin is an endogenous peptide hormone almost exclusively expressed in the human gastrointestinal (GI) tract. It activates the motilin receptor (MTLR), a class A G protein-coupled receptor (GPCR), and stimulates GI motility. To our knowledge, MTLR is the first GPCR reported to be activated by macrolide antibiotics, such as erythromycin. It has attracted extensive attention as a potential drug target for GI disorders. We report two structures of Gq-coupled human MTLR bound to motilin and erythromycin. Our structures reveal the recognition mechanism of both ligands and explain the specificity of motilin and ghrelin, a related gut peptide hormone, for their respective receptors. These structures also provide the... More

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