Nature Communications (Aug 2022)
Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
- Elizaveta Lyapina,
- Egor Marin,
- Anastasiia Gusach,
- Philipp Orekhov,
- Andrey Gerasimov,
- Aleksandra Luginina,
- Daniil Vakhrameev,
- Margarita Ergasheva,
- Margarita Kovaleva,
- Georgii Khusainov,
- Polina Khorn,
- Mikhail Shevtsov,
- Kirill Kovalev,
- Sergey Bukhdruker,
- Ivan Okhrimenko,
- Petr Popov,
- Hao Hu,
- Uwe Weierstall,
- Wei Liu,
- Yunje Cho,
- Ivan Gushchin,
- Andrey Rogachev,
- Gleb Bourenkov,
- Sehan Park,
- Gisu Park,
- Hyo Jung Hyun,
- Jaehyun Park,
- Valentin Gordeliy,
- Valentin Borshchevskiy,
- Alexey Mishin,
- Vadim Cherezov
Affiliations
- Elizaveta Lyapina
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Egor Marin
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Anastasiia Gusach
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Philipp Orekhov
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Andrey Gerasimov
- Vyatka State University
- Aleksandra Luginina
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Daniil Vakhrameev
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Margarita Ergasheva
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Margarita Kovaleva
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Georgii Khusainov
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Polina Khorn
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Mikhail Shevtsov
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Kirill Kovalev
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Sergey Bukhdruker
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Ivan Okhrimenko
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Petr Popov
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Hao Hu
- Department of Physics, Arizona State University
- Uwe Weierstall
- Department of Physics, Arizona State University
- Wei Liu
- Cancer Center and Department of Pharmacology and Toxicology, Medical College of Wisconsin
- Yunje Cho
- Department of Life Science, Pohang University of Science and Technology
- Ivan Gushchin
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Andrey Rogachev
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Gleb Bourenkov
- European Molecular Biology Laboratory, Hamburg unit c/o DESY
- Sehan Park
- Pohang Accelerator Laboratory, POSTECH
- Gisu Park
- Pohang Accelerator Laboratory, POSTECH
- Hyo Jung Hyun
- Pohang Accelerator Laboratory, POSTECH
- Jaehyun Park
- Pohang Accelerator Laboratory, POSTECH
- Valentin Gordeliy
- Institut de Biologie Structurale (IBS), Université Grenoble Alpes, CEA, CNRS
- Valentin Borshchevskiy
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Alexey Mishin
- Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and Technology
- Vadim Cherezov
- Bridge Institute, Department of Chemistry, University of Southern California
- DOI
- https://doi.org/10.1038/s41467-022-32447-1
- Journal volume & issue
-
Vol. 13,
no. 1
pp. 1 – 14
Abstract
S1P5 is a sphingosine-1-phosphate (S1P) receptor implicated in immune and neurodegenerative disorders. Here, authors report a crystal structure of the S1P5 receptor in complex with a selective inverse agonist, revealing an allosteric subpocket and shedding light on inverse agonism in S1P receptors.
