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TitleCryo-EM structure of the β3-adrenergic receptor reveals the molecular basis of subtype selectivity.
Journal, issue, pagesMol Cell, Vol. 81, Issue 15, Page 3205-33215.e5, Year 2021
Publish dateAug 5, 2021
AuthorsChisae Nagiri / Kazuhiro Kobayashi / Atsuhiro Tomita / Masahiko Kato / Kan Kobayashi / Keitaro Yamashita / Tomohiro Nishizawa / Asuka Inoue / Wataru Shihoya / Osamu Nureki /
PubMed AbstractThe 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.
External linksMol Cell / PubMed:34314699
MethodsEM (single particle)
Resolution3.16 - 3.3 Å
Structure data

30678

7dh5

EMDB-30678, PDB-7dh5:
Dog beta3 adrenergic receptor bound to mirabegron in complex with a miniGs heterotrimer
Method: EM (single particle) / Resolution: 3.16 Å

33227

7xjh

EMDB-33227, PDB-7xjh:
Isoproterenol-activated dog beta3 adrenergic receptor
Method: EM (single particle) / Resolution: 3.3 Å

Chemicals

ChemComp-H6U:
2-(2-azanyl-1,3-thiazol-4-yl)-N-[4-[2-[[(2R)-2-oxidanyl-2-phenyl-ethyl]amino]ethyl]phenyl]ethanamide / medication*YM / Mirabegron

ChemComp-5FW:
ISOPRENALINE / medication, agonist*YM / Isoprenaline

Source
  • homo sapiens (human)
  • rattus norvegicus (Norway rat)
  • bos taurus (cattle)
  • unidentified (others)
  • canis lupus familiaris (dog)
KeywordsMEMBRANE PROTEIN / GPCR

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