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Fluorescent agonists and antagonists for vasopressin/oxytocin G protein-coupled receptors: Usefulness in ligand screening assays and receptor studies

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2008)

期刊

MINI-REVIEWS IN MEDICINAL CHEMISTRY

卷 8, 期 10, 页码 996-1005

出版社

BENTHAM SCIENCE PUBL LTD

DOI: 10.2174/138955708785740607

关键词

arginine-vasopressin; oxytocin; G protein-coupled receptor; structure-activity relationships; fluorescent peptide; fluorescence resonance energy transfer; fluorescence polarization; high-throughput screening assays

类别

Chemistry, Medicinal

资金

NIGMS NIH HHS [R01 GM025280, GM25280] Funding Source: Medline

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Protocol

Reagent

摘要

Different series of fluorescent agonists and antagonists have been developed and characterized for argininevasopressin and oxytocin G protein-coupled receptors. Both cyclic and linear peptide analogs of the neurohypophysial hormones are useful tools for investigating receptor localization and trafficking, analysing receptor structural organization, and developing new receptor-selective high-throughput ligand screening assays.

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Laura Droctove, Manon Lancien, Vu Long Tran, Michael Susset, Benoit Jego, Frederic Theodoro, Pascal Kessler, Gilles Mourier, Philippe Robin, Sekou Siramakan Diarra, Stefano Palea, Adrien Flahault, Amelia Chorfa, Maithe Corbani, Catherine Llorens-Cortes, Bernard Mouillac, Christiane Mendre, Alain Pruvost, Denis Servent, Charles Truillet, Nicolas Gilles

THERANOSTICS (2020)

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Meeting Abstract Biophysics

Mechanims of activation of the mu-opoid and the vasopressin V2 receptors seen by liquid NMR

H. Demene, R. Sounier, T. Laeremans, H. Orcel, J. Steyaert, A. Manglik, B. Kobilka, B. Mouillac, S. Granier

EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS (2019)

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