Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
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.
| Main Authors: | , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Nature Portfolio
2022-08-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/s41467-022-32447-1 |
| _version_ | 1811215899213955072 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Elizaveta Lyapina |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-12T06:30:04Z |
| format | Article |
| id | doaj.art-36cf9a61df10484aabf068185a39d283 |
| institution | Directory Open Access Journal |
| issn | 2041-1723 |
| language | English |
| last_indexed | 2024-04-12T06:30:04Z |
| publishDate | 2022-08-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Nature Communications |
| spelling | doaj.art-36cf9a61df10484aabf068185a39d2832022-12-22T03:44:02ZengNature PortfolioNature Communications2041-17232022-08-0113111410.1038/s41467-022-32447-1Structural basis for receptor selectivity and inverse agonism in S1P5 receptorsElizaveta Lyapina0Egor Marin1Anastasiia Gusach2Philipp Orekhov3Andrey Gerasimov4Aleksandra Luginina5Daniil Vakhrameev6Margarita Ergasheva7Margarita Kovaleva8Georgii Khusainov9Polina Khorn10Mikhail Shevtsov11Kirill Kovalev12Sergey Bukhdruker13Ivan Okhrimenko14Petr Popov15Hao Hu16Uwe Weierstall17Wei Liu18Yunje Cho19Ivan Gushchin20Andrey Rogachev21Gleb Bourenkov22Sehan Park23Gisu Park24Hyo Jung Hyun25Jaehyun Park26Valentin Gordeliy27Valentin Borshchevskiy28Alexey Mishin29Vadim Cherezov30Research Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyVyatka State UniversityResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyDepartment of Physics, Arizona State UniversityDepartment of Physics, Arizona State UniversityCancer Center and Department of Pharmacology and Toxicology, Medical College of WisconsinDepartment of Life Science, Pohang University of Science and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyEuropean Molecular Biology Laboratory, Hamburg unit c/o DESYPohang Accelerator Laboratory, POSTECHPohang Accelerator Laboratory, POSTECHPohang Accelerator Laboratory, POSTECHPohang Accelerator Laboratory, POSTECHInstitut de Biologie Structurale (IBS), Université Grenoble Alpes, CEA, CNRSResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyResearch Сenter for Molecular Mechanisms of Aging and Age-related Diseases, Moscow Institute of Physics and TechnologyBridge Institute, Department of Chemistry, University of Southern CaliforniaS1P5 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.https://doi.org/10.1038/s41467-022-32447-1 |
| spellingShingle | 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 Structural basis for receptor selectivity and inverse agonism in S1P5 receptors Nature Communications |
| title | Structural basis for receptor selectivity and inverse agonism in S1P5 receptors |
| title_full | Structural basis for receptor selectivity and inverse agonism in S1P5 receptors |
| title_fullStr | Structural basis for receptor selectivity and inverse agonism in S1P5 receptors |
| title_full_unstemmed | Structural basis for receptor selectivity and inverse agonism in S1P5 receptors |
| title_short | Structural basis for receptor selectivity and inverse agonism in S1P5 receptors |
| title_sort | structural basis for receptor selectivity and inverse agonism in s1p5 receptors |
| url | https://doi.org/10.1038/s41467-022-32447-1 |
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