Ontology highlight
ABSTRACT:
SUBMITTER: Wagner G
PROVIDER: S-EPMC6943558 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Wágner Gábor G Mocking Tamara A M TAM Kooistra Albert J AJ Slynko Inna I Ábrányi-Balogh Péter P Keserű György M GM Wijtmans Maikel M Vischer Henry F HF de Esch Iwan J P IJP Leurs Rob R
Molecules (Basel, Switzerland) 20191211 24
Covalent binding of G protein-coupled receptors by small molecules is a useful approach for better understanding of the structure and function of these proteins. We designed, synthesized and characterized a series of 6 potential covalent ligands for the histamine H<sub>3</sub> receptor (H<sub>3</sub>R). Starting from a 2-amino-pyrimidine scaffold, optimization of anchor moiety and warhead followed by fine-tuning of the required reactivity via scaffold hopping resulted in the isothiocyanate H<sub ...[more]