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TitleLigand recognition, unconventional activation, and G protein coupling of the prostaglandin E receptor EP2 subtype.
Journal, issue, pagesSci Adv, Vol. 7, Issue 14, Year 2021
Publish dateApr 2, 2021
AuthorsChangxiu Qu / Chunyou Mao / Peng Xiao / Qingya Shen / Ya-Ni Zhong / Fan Yang / Dan-Dan Shen / Xiaona Tao / Huibing Zhang / Xu Yan / Ru-Jia Zhao / Junyan He / Ying Guan / Chao Zhang / Guihua Hou / Peng-Ju Zhang / Guige Hou / Zijian Li / Xiao Yu / Ren-Jie Chai / You-Fei Guan / Jin-Peng Sun / Yan Zhang /
PubMed AbstractSelective modulation of the heterotrimeric G protein α S subunit-coupled prostaglandin E (PGE) receptor EP2 subtype is a promising therapeutic strategy for osteoporosis, ocular hypertension, ...Selective modulation of the heterotrimeric G protein α S subunit-coupled prostaglandin E (PGE) receptor EP2 subtype is a promising therapeutic strategy for osteoporosis, ocular hypertension, neurodegenerative diseases, and cardiovascular disorders. Here, we report the cryo-electron microscopy structure of the EP2-G complex with its endogenous agonist PGE and two synthesized agonists, taprenepag and evatanepag (CP-533536). These structures revealed distinct features of EP2 within the EP receptor family in terms of its unconventional receptor activation and G protein coupling mechanisms, including activation in the absence of a typical W "toggle switch" and coupling to G via helix 8. Moreover, inspection of the agonist-bound EP2 structures uncovered key motifs governing ligand selectivity. Our study provides important knowledge for agonist recognition and activation mechanisms of EP2 and will facilitate the rational design of drugs targeting the PGE signaling system.
External linksSci Adv / PubMed:33811074 / PubMed Central
MethodsEM (single particle)
Resolution2.8 - 2.9 Å
Structure data

30489

7cx2

EMDB-30489, PDB-7cx2:
Cryo-EM structure of the PGE2-bound EP2-Gs complex
Method: EM (single particle) / Resolution: 2.8 Å

30490

7cx3

EMDB-30490, PDB-7cx3:
Cryo-EM structure of the Taprenepag-bound EP2-Gs complex
Method: EM (single particle) / Resolution: 2.8 Å

30491

7cx4

EMDB-30491, PDB-7cx4:
Cryo-EM structure of the Evatanepag-bound EP2-Gs complex
Method: EM (single particle) / Resolution: 2.9 Å

Chemicals

ChemComp-P2E:
(Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxo-cyclopentyl]hept-5-enoic acid / medication*YM

ChemComp-HOH:
WATER

ChemComp-GNO:
2-[3-[[(4-pyrazol-1-ylphenyl)methyl-pyridin-3-ylsulfonyl-amino]methyl]phenoxy]ethanoic acid

ChemComp-GM9:
2-[3-[[(4-~{tert}-butylphenyl)methyl-pyridin-3-ylsulfonyl-amino]methyl]phenoxy]ethanoic acid

Source
  • homo sapiens (human)
  • synthetic construct (others)
KeywordsMEMBRANE PROTEIN / GPCR / EP2 / Complex / PGE2 / Taprenepag / Evatanepag

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