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Importance of the second extracellular loop for melatonin MT 1 receptor function and absence of melatonin binding in GPR50
Author(s) -
Clement Nathalie,
Renault Nicolas,
Guillaume JeanLuc,
Cecon Erika,
Journé AnneSophie,
Laurent Xavier,
Tadagaki Kenjiro,
Cogé Francis,
Gohier Arnaud,
Delagrange Philippe,
Chavatte Philippe,
Jockers Ralf
Publication year - 2018
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.14029
Subject(s) - melatonin receptor , receptor , melatonin , g protein coupled receptor , biophysics , biology , microbiology and biotechnology , transmembrane domain , chemistry , biochemistry , neuroscience
Recent crystal structures of GPCRs have emphasized the previously unappreciated role of the second extracellular (E2) loop in ligand binding and gating and receptor activation. Here, we have assessed the role of the E2 loop in the activation of the melatonin MT 1 receptor and in the inactivation of the closely related orphan receptor GPR50.