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Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein


ABSTRACT:

SUBMITTER: Wataru Shihoya 

PROVIDER: EMPIAR-10351 | biostudies-other |

REPOSITORIES: biostudies-other

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Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein.

Kobayashi Kazuhiro K   Shihoya Wataru W   Nishizawa Tomohiro T   Kadji Francois Marie Ngako FMN   Aoki Junken J   Inoue Asuka A   Nureki Osamu O  

Nature structural & molecular biology 20200309 3


Pituitary adenylate cyclase-activating polypeptide (PACAP) is a pleiotropic neuropeptide hormone. The PACAP receptor PAC1R, which belongs to the class B G-protein-coupled receptors (GPCRs), is a drug target for mental disorders and dry eye syndrome. Here, we present a cryo-EM structure of human PAC1R bound to PACAP and an engineered G<sub>s</sub> heterotrimer. The structure revealed that transmembrane helix TM1 plays an essential role in PACAP recognition. The extracellular domain (ECD) of PAC1R  ...[more]

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