Crystal structure reveals the binding mode and selectivity of a photoswitchable ligand for the adenosine A2A receptor
Copyright © 2023 The Authors. Published by Elsevier Inc. All rights reserved..
Rational synthetic expansion of photoresponsive ligands is important for photopharmacological studies. Adenosine A2A receptor (A2AR) is stimulated by adenosine and related in Parkinson's disease and other diseases. Here, we report the crystal structure of the A2AR in complex with the novel photoresponsive ligand photoNECA (blue) at 3.34 Å resolution. PhotoNECA (blue) was designed for this structural study and the cell-based assay showed a photoresponsive and receptor selective characteristics of photoNECA (blue) for A2AR. The crystal structure explains the binding mode, photoresponsive mechanism and receptor selectivity of photoNECA (blue). Our study would promote not only the rational design of photoresponsive ligands but also dynamic structural studies of A2AR.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:695 |
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| Enthalten in: |
Biochemical and biophysical research communications - 695(2024) vom: 05. Feb., Seite 149393 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Araya, Tsuyoshi [VerfasserIn] |
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| Links: |
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| Themen: |
Adenosine |
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| Anmerkungen: |
Date Completed 06.02.2024 Date Revised 06.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bbrc.2023.149393 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Rational synthetic expansion of photoresponsive ligands is important for photopharmacological studies. Adenosine A2A receptor (A2AR) is stimulated by adenosine and related in Parkinson's disease and other diseases. Here, we report the crystal structure of the A2AR in complex with the novel photoresponsive ligand photoNECA (blue) at 3.34 Å resolution. PhotoNECA (blue) was designed for this structural study and the cell-based assay showed a photoresponsive and receptor selective characteristics of photoNECA (blue) for A2AR. The crystal structure explains the binding mode, photoresponsive mechanism and receptor selectivity of photoNECA (blue). Our study would promote not only the rational design of photoresponsive ligands but also dynamic structural studies of A2AR | ||
| 650 | 4 | |a Journal Article | |
| 650 | 7 | |a Adenosine |2 NLM | |
| 650 | 7 | |a K72T3FS567 |2 NLM | |
| 650 | 7 | |a Ligands |2 NLM | |
| 650 | 7 | |a Receptor, Adenosine A2A |2 NLM | |
| 650 | 7 | |a Fluorescent Dyes |2 NLM | |
| 700 | 1 | |a Matsuba, Yuya |e verfasserin |4 aut | |
| 700 | 1 | |a Suzuki, Harufumi |e verfasserin |4 aut | |
| 700 | 1 | |a Doura, Tomohiro |e verfasserin |4 aut | |
| 700 | 1 | |a Nuemket, Nipawan |e verfasserin |4 aut | |
| 700 | 1 | |a Nango, Eriko |e verfasserin |4 aut | |
| 700 | 1 | |a Yamamoto, Masaki |e verfasserin |4 aut | |
| 700 | 1 | |a Im, Dohyun |e verfasserin |4 aut | |
| 700 | 1 | |a Asada, Hidetsugu |e verfasserin |4 aut | |
| 700 | 1 | |a Kiyonaka, Shigeki |e verfasserin |4 aut | |
| 700 | 1 | |a Iwata, So |e verfasserin |4 aut | |
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