Solid-state NMR evidence for a protonation switch in the binding pocket of the H1 receptor upon binding of the agonist histamine

V.R. Ratnala, S.R. Kiihne, F. Buda, R. Leurs, H. de Groot, W.J. DeGrip

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

G protein coupled receptors (GPCRs) represent a major superfamily of transmembrane receptor proteins that are crucial in cellular signaling and are major pharmacological targets. While the activity of GPCRs can be modulated by agonist binding, the mechanisms that link agonist binding to G protein coupling are poorly understood. Here we present a method to accurately examine the activity of ligands in their bound state, even at low affinity, by solid-state NMR dipolar correlation spectroscopy and confront this method with the human H
Original languageEnglish
Pages (from-to)867-72
JournalJournal of the American Chemical Society
Volume129
Issue number4
DOIs
Publication statusPublished - 2007

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