@article{f79b9370046b4977b220b4b4eb4702e2,
title = "Crystal structure of the endogenous agonist-bound prostanoid receptor EP3",
abstract = " Prostanoids are a series of bioactive lipid metabolites that function in an autacoid manner via activation of cognate G-protein-coupled receptors (GPCRs). Here, we report the crystal structure of human prostaglandin (PG) E receptor subtype EP3 bound to endogenous ligand PGE 2 at 2.90 {\AA} resolution. The structure reveals important insights into the activation mechanism of prostanoid receptors and provides a molecular basis for the binding modes of endogenous ligands. ",
author = "Kazushi Morimoto and Ryoji Suno and Yunhong Hotta and Keitaro Yamashita and Kunio Hirata and Masaki Yamamoto and Shuh Narumiya and So Iwata and Takuya Kobayashi",
note = "Funding Information: This work was supported by AMED under grant Numbers JP18gm0910007 (CREST; T.K.) and JP18am0101079 (S.I.), JP18am0101070 (M.Y.) (Platform Project for Supporting Drug Discovery and Life Science Research; Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) and JSPS KAKENHI grant Number 15J00102 (K.M.). The authors acknowledge support from the Toray Science Foundation (T.K.), Takeda Science Foundation (R.S. and T.K.), Naito Foundation (T.K.), and Koyanagi Foundation (T.K.). The synchrotron radiation experiments were performed at BL32XU of SPring-8 with the approval of the Japan Synchrotron Radiation Research Institute (JASRI) (Proposal No. 2017A2524, 2017B2524, and BINDS0483). We thank the staff members of BL32XU for help with X-ray data collection. DNA sequencing analysis was performed at the Medical Research Support Center, Graduate School of Medicine, Kyoto University. We are grateful to A. Inoue for providing instruction on the TGFα shedding assay, M. Shiroishi for providing instruction on FSEC-TS, D. Im and T. Shimamura (Kyoto University) for providing the plasmid encoding mbIIG2, S. Horita for support for structure refinement, and H. Tsujimoto and M. Sasanuma for technical assistance. Publisher Copyright: {\textcopyright} 2018, The Author(s), under exclusive licence to Springer Nature America, Inc.",
year = "2019",
month = jan,
day = "1",
doi = "10.1038/s41589-018-0171-8",
language = "English",
volume = "15",
pages = "8--10",
journal = "Nature Chemical Biology",
issn = "1552-4450",
publisher = "Nature Publishing Group",
number = "1",
}