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Structure of the agonist 12–HHT in its BLT2 receptor-bound state

Authors
  • Giusti, Fabrice1, 2
  • Casiraghi, Marina1, 3
  • Point, Elodie1
  • Damian, Marjorie4
  • Rieger, Jutta5
  • Bon, Christel Le1
  • Pozza, Alexandre1
  • Moncoq, Karine1
  • Banères, Jean-Louis4
  • Catoire, Laurent J.1
  • 1 Laboratoire de Biologie Physico-Chimique des Protéines Membranaires, UMR 7099, CNRS/Université de Paris, Institut de Biologie Physico–Chimique (FRC 550), 13 rue Pierre et Marie Curie, Paris, F–75005, France , Paris (France)
  • 2 Institut de Chimie Séparative de Marcoule, ICSM UMR 5257, Site de Marcoule, Bâtiment 426, BP 17171, Bagnols sur Cèze Cedex, F-30207, France , Bagnols sur Cèze Cedex (France)
  • 3 Stanford University School of Medicine, 279 Campus Drive, Stanford California, 94305, USA , Stanford California (United States)
  • 4 Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, Université Montpellier, ENSCM, , 15 av. Charles Flahault, Montpellier, 34093, France , Montpellier (France)
  • 5 Institut Parisien de Chimie Moléculaire, Sorbonne Université, CNRS, UMR 8232, Equipe Chimie des Polymères, 4 place Jussieu, 75252, Paris Cedex, 05, France , Paris Cedex (France)
Type
Published Article
Journal
Scientific Reports
Publisher
Springer Nature
Publication Date
Feb 14, 2020
Volume
10
Issue
1
Identifiers
DOI: 10.1038/s41598-020-59571-6
Source
Springer Nature
License
Green

Abstract

G Protein-Coupled receptors represent the main communicating pathway for signals from the outside to the inside of most of eukaryotic cells. They define the largest family of integral membrane receptors at the surface of the cells and constitute the main target of the current drugs on the market. The low affinity leukotriene receptor BLT2 is a receptor involved in pro- and anti-inflammatory pathways and can be activated by various unsaturated fatty acid compounds. We present here the NMR structure of the agonist 12–HHT in its BLT2-bound state and a model of interaction of the ligand with the receptor based on a conformational homology modeling associated with docking simulations. Put into perspective with the data obtained with leukotriene B4, our results illuminate the ligand selectivity of BLT2 and may help define new molecules to modulate the activity of this receptor.

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