Crystal structure of the endogenous agonist-bound prostanoid receptor EP3

被引：47

作者：

Morimoto, Kazushi ^{[1
,2
]}

Suno, Ryoji ^{[1
,2
]}

Hotta, Yunhong ^{[1
]}

Yamashita, Keitaro ^{[3
]}

Hirata, Kunio ^{[3
]}

Yamamoto, Masaki ^{[3
]}

Narumiya, Shuh ^{[4
]}

Iwata, So ^{[1
]}

Kobayashi, Takuya ^{[1
,2
,5
]}

机构：

[1] Kyoto Univ, Dept Cell Biol, Grad Sch Med, Sakyo Ku, Konoe Cho, Kyoto, Japan

[2] Japan Agcy Med Res & Dev AMED, CREST, Chiyoda Ku, Tokyo, Japan

[3] RIKEN, SPring Ctr 8, Sayo, Hyogo, Japan

[4] Kyoto Univ, Med Innovat Ctr, Grad Sch Med, Sakyo Ku, Kyoto, Japan

[5] Kansai Med Univ, Dept Med Chem, Hirakata, Osaka, Japan

来源：

NATURE CHEMICAL BIOLOGY | 2019年 / 15卷 / 01期

关键词：

SITE-DIRECTED MUTAGENESIS; PROTEIN; ASSAY;

D O I：

10.1038/s41589-018-0171-8

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 angstrom 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.

引用

页码：8 / +

页数：8

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