Cell‐permeable high‐affinity tracers for G q proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors

ISSN
0007-1188
1476-5381
Date Issued
2020
Author(s)
Kuschak, Markus
Namasivayam, Vigneshwaran
Voss, Jan H.
Garg, Jaspal
Schlegel, Jonathan G.
Abdelrahman, Aliaa
Kehraus, Stefan
Reher, Raphael
Küppers, Jim
Sylvester, Katharina
Hinz, Sonja
Matthey, Michaela
Wenzel, Daniela
Fleischmann, Bernd K.
Pfeifer, Alexander
Inoue, Asuka
Gütschow, Michael
König, Gabriele M.
Müller, Christa E.
DOI
10.1111/bph.14960
Abstract
G proteins are intracellular switches that transduce and amplify extracellular signals from GPCRs. The Gq protein subtypes, which are coupled to PLC activation, can act as oncogenes, and their expression was reported to be up-regulated in cancer and inflammatory diseases. Gq inhibition may be an efficient therapeutic strategy constituting a new level of intervention. However, diagnostic tools and therapeutic drugs for Gq proteins are lacking.