- EMDB-30678: Dog beta3 adrenergic receptor bound to mirabegron in complex with... -
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Entry
Database: EMDB / ID: EMD-30678
Title
Dog beta3 adrenergic receptor bound to mirabegron in complex with a miniGs heterotrimer
Map data
Sample
Complex: Dog beta3 adrenergic receptor bound to mirabegron in complex with a miniGs heterotrimer
Complex: Guanine nucleotide-binding protein G(s) subunit alpha isoforms short
Protein or peptide: Guanine nucleotide-binding protein G(s) subunit alpha isoforms short,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short
Complex: Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
Protein or peptide: Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
Complex: Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Protein or peptide: Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Journal: Mol Cell / Year: 2021 Title: Cryo-EM structure of the β3-adrenergic receptor reveals the molecular basis of subtype selectivity. Authors: Chisae Nagiri / Kazuhiro Kobayashi / Atsuhiro Tomita / Masahiko Kato / Kan Kobayashi / Keitaro Yamashita / Tomohiro Nishizawa / Asuka Inoue / Wataru Shihoya / Osamu Nureki / Abstract: The β-adrenergic receptor (βAR) is predominantly expressed in adipose tissue and urinary bladder and has emerged as an attractive drug target for the treatment of type 2 diabetes, obesity, and ...The β-adrenergic receptor (βAR) is predominantly expressed in adipose tissue and urinary bladder and has emerged as an attractive drug target for the treatment of type 2 diabetes, obesity, and overactive bladder (OAB). Here, we report the cryogenic electron microscopy structure of the βAR-G signaling complex with the selective agonist mirabegron, a first-in-class drug for OAB. Comparison of this structure with the previously reported βAR and βAR structures reveals a receptor activation mechanism upon mirabegron binding to the orthosteric site. Notably, the narrower exosite in βAR creates a perpendicular pocket for mirabegron. Mutational analyses suggest that a combination of both the exosite shape and the amino-acid-residue substitutions defines the drug selectivity of the βAR agonists. Our findings provide a molecular basis for βAR subtype selectivity, allowing the design of more-selective agents with fewer adverse effects.
History
Deposition
Nov 12, 2020
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Header (metadata) release
Aug 4, 2021
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Map release
Aug 4, 2021
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Update
Aug 18, 2021
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Current status
Aug 18, 2021
Processing site: PDBj / Status: Released
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Entire : Dog beta3 adrenergic receptor bound to mirabegron in complex with...
Entire
Name: Dog beta3 adrenergic receptor bound to mirabegron in complex with a miniGs heterotrimer
Components
Complex: Dog beta3 adrenergic receptor bound to mirabegron in complex with a miniGs heterotrimer
Complex: Guanine nucleotide-binding protein G(s) subunit alpha isoforms short
Protein or peptide: Guanine nucleotide-binding protein G(s) subunit alpha isoforms short,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short
Complex: Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
Protein or peptide: Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
Complex: Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Protein or peptide: Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
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