Cell-permeable high-affinity tracers for Gq proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors.

Markus KuschakVigneshwaran Namasivayam Muhammad Rafehi Jan Hendrik VoßJaspal GargJonathan G SchlegelAliaa AbdelrahmanStefan KehrausRaphael ReherJim KüppersKatharina SylvesterSonja HinzMichaela Matthey Daniela Wenzel Bernd K FleischmannAlexander PfeiferAsuka InoueMichael Gütschow Gabriele M König Christa Elisabeth Müller

Published in: British journal of pharmacology (2020)

The Gq protein inhibitors YM and FR are pharmacologically different despite similar structures. The new versatile tools and powerful assays will contribute to the advancement of the rising field of G protein research.

Keyphrases

small molecule
single cell
protein protein
binding protein
cell therapy
high resolution
genome wide
gene expression
bone marrow
transcription factor