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TitleStructural insights into ligand recognition, activation, and signaling of the α adrenergic receptor.
Journal, issue, pagesSci Adv, Vol. 8, Issue 9, Page eabj5347, Year 2022
Publish dateMar 4, 2022
AuthorsJun Xu / Sheng Cao / Harald Hübner / Dorothée Weikert / Geng Chen / Qiuyuan Lu / Daopeng Yuan / Peter Gmeiner / Zheng Liu / Yang Du /
PubMed AbstractThe α adrenergic receptor (αAR) is a G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptor that mediates important physiological functions in response to the endogenous ...The α adrenergic receptor (αAR) is a G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptor that mediates important physiological functions in response to the endogenous neurotransmitters norepinephrine and epinephrine, as well as numerous chemically distinct drugs. However, the molecular mechanisms of drug actions remain poorly understood. Here, we report the cryo-electron microscopy structures of the human αAR-GoA complex bound to norepinephrine and three imidazoline derivatives (brimonidine, dexmedetomidine, and oxymetazoline). Together with mutagenesis and functional data, these structures provide important insights into the molecular basis of ligand recognition, activation, and signaling at the αAR. Further structural analyses uncover different molecular determinants between αAR and βARs for recognition of norepinephrine and key regions that determine the G protein coupling selectivity. Overall, our studies provide a framework for understanding the signal transduction of the adrenergic system at the atomic level, which will facilitate rational structure-based discovery of safer and more effective medications for αAR.
External linksSci Adv / PubMed:35245122 / PubMed Central
MethodsEM (single particle)
Resolution3.0 - 3.6 Å
Structure data

31147

7ej0

EMDB-31147, PDB-7ej0:
Structure of the alpha2A-adrenergic receptor GoA signaling complex
Method: EM (single particle) / Resolution: 3.2 Å

31156

7ej8

EMDB-31156, PDB-7ej8:
Structure of the alpha2A-adrenergic receptor GoA signaling complex bound to brimonidine
Method: EM (single particle) / Resolution: 3.0 Å

31157

7eja

EMDB-31157, PDB-7eja:
Structure of the alpha2A-adrenergic receptor GoA signaling complex bound to dexmedetomidine
Method: EM (single particle) / Resolution: 3.6 Å

31162

7ejk

EMDB-31162, PDB-7ejk:
Structure of the alpha2A-adrenergic receptor GoA signaling complex bound to oxymetazoline
Method: EM (single particle) / Resolution: 3.4 Å

Chemicals

ChemComp-E5E:
Noradrenaline / neurotransmitter, hormone*YM / Norepinephrine

ChemComp-J59:
Brimonidine / medication, agonist*YM / Brimonidine

ChemComp-CZX:
4-[(1~{S})-1-(2,3-dimethylphenyl)ethyl]-1~{H}-imidazole / Dexmedetomidine

ChemComp-J5C:
Oxymetazoline / medication*YM / Oxymetazoline

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / alpha2A-adrenergic receptor / signaling complex / cryo-EM

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