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6K41

cryo-EM structure of alpha2BAR-GoA complex

Summary for 6K41
Entry DOI10.2210/pdb6k41/pdb
EMDB information9911 9912
DescriptorGuanine nucleotide-binding protein G(o) subunit alpha, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... (6 entities in total)
Functional Keywordsgpcr, complex, cryo-em, membrane protein
Biological sourceHomo sapiens (Human)
More
Total number of polymer chains5
Total formula weight177619.78
Authors
Yuan, D.,Liu, Z.,Wang, H.W.,Kobilka, B.K. (deposition date: 2019-05-23, release date: 2020-04-15, Last modification date: 2020-05-13)
Primary citationYuan, D.,Liu, Z.,Kaindl, J.,Maeda, S.,Zhao, J.,Sun, X.,Xu, J.,Gmeiner, P.,Wang, H.W.,Kobilka, B.K.
Activation of the alpha2Badrenoceptor by the sedative sympatholytic dexmedetomidine.
Nat.Chem.Biol., 16:507-512, 2020
Cited by
PubMed Abstract: The α adrenergic receptors (αARs) are G protein-coupled receptors (GPCRs) that respond to adrenaline and noradrenaline and couple to the Gi/o family of G proteins. αARs play important roles in regulating the sympathetic nervous system. Dexmedetomidine is a highly selective αAR agonist used in post-operative patients as an anxiety-reducing, sedative medicine that decreases the requirement for opioids. As is typical for selective αAR agonists, dexmedetomidine consists of an imidazole ring and a substituted benzene moiety lacking polar groups, which is in contrast to βAR-selective agonists, which share an ethanolamine group and an aromatic system with polar, hydrogen-bonding substituents. To better understand the structural basis for the selectivity and efficacy of adrenergic agonists, we determined the structure of the αAR in complex with dexmedetomidine and Go at a resolution of 2.9 Å by single-particle cryo-EM. The structure reveals the mechanism of αAR-selective activation and provides insights into Gi/o coupling specificity.
PubMed: 32152538
DOI: 10.1038/s41589-020-0492-2
PDB entries with the same primary citation
Experimental method
ELECTRON MICROSCOPY (2.9 Å)
Structure validation

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