Endogenous agonist–bound S1PR3 structure reveals determinants of G protein

Endogenous agonist–bound S1PR3 structure reveals determinants of G protein–subtype bias

Published:2021-06-11 Issue:24 Volume:7 Page:
ISSN:2375-2548
Container-title:Science Advances
language:en
Short-container-title:Sci. Adv.

Author:

Maeda Shintaro¹²^ORCID,Shiimura Yuki³⁴^ORCID,Asada Hidetsugu³^ORCID,Hirata Kunio⁵^ORCID,Luo Fangjia³⁵^ORCID,Nango Eriko³⁵⁶^ORCID,Tanaka Nobuo⁷^ORCID,Toyomoto Masayasu¹⁸^ORCID,Inoue Asuka⁹,Aoki Junken⁹^ORCID,Iwata So³⁵^ORCID,Hagiwara Masatoshi¹²⁷⁸^ORCID

Affiliation:

1. Department of Anatomy and Developmental Biology, Graduate School of Medicine, Kyoto University, Kyoto 606-8501, Japan.

2. Department of Drug Discovery Medicine, Graduate School of Medicine, Kyoto University, Sakyo-ku, Kyoto 606-8507, Japan.

3. Department of Cell Biology, Graduate School of Medicine, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.

4. Institute of Life Science, Kurume University, Kurume, Fukuoka 830-0011, Japan.

5. RIKEN SPring-8 Center, Sayo-cho, Sayo-gun, Hyogo 679-5165, Japan.

6. Institute of Multidisciplinary Research for Advanced Materials, Tohoku University, 2-1-1 Katahira, Aoba-ku, Sendai 980-8577, Japan.

7. Medical Research Support Center, Graduate School of Medicine, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.

8. Department of Drug Discovery for Lung Diseases, Graduate School of Medicine, Kyoto University, Kyoto 606-8501, Japan.

9. Laboratory of Molecular and Cellular Biochemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi 980-8578, Japan.

Abstract

Active S1PR3 structure reveals the unique ligand-binding mode and signaling selectivity switching mechanism.

Funder

Japan Agency for Medical Research and Development

Japan Society for the Promotion of Science

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

Reference54 articles.

1. The Molecular Basis of G Protein–Coupled Receptor Activation

2. G Protein Pathways

3. Heterotrimeric G protein activation by G-protein-coupled receptors

4. Generic GPCR residue numbers – aligning topology maps while minding the gaps

5. Functional Selectivity and Classical Concepts of Quantitative Pharmacology

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