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Dog beta3 adrenergic receptor bound to mirabegron in complex with a miniGs heterotrimer


ABSTRACT:

SUBMITTER: Osamu Nureki 

PROVIDER: EMPIAR-11352 | biostudies-other |

REPOSITORIES: biostudies-other

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Cryo-EM structure of the β3-adrenergic receptor reveals the molecular basis of subtype selectivity.

Nagiri Chisae C   Kobayashi Kazuhiro K   Tomita Atsuhiro A   Kato Masahiko M   Kobayashi Kan K   Yamashita Keitaro K   Nishizawa Tomohiro T   Inoue Asuka A   Shihoya Wataru W   Nureki Osamu O  

Molecular cell 20210726 15


The β<sub>3</sub>-adrenergic receptor (β<sub>3</sub>AR) 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 β<sub>3</sub>AR-G<sub>s</sub> signaling complex with the selective agonist mirabegron, a first-in-class drug for OAB. Comparison of this structure with the previously reported β<sub>1</sub>A  ...[more]

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