Biochemical and Biophysical Research Communications 2016-01-01

G-protein inhibition profile of the reported Gq/11 inhibitor UBO-QIC.

Jyrki P Kukkonen

Index: Biochem. Biophys. Res. Commun. 469 , 101-7, (2015)

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Abstract

UBO-QIC (FR900359) is the only currently available Gq/11 protein inhibitor. However, its characterization has not been published, and we thus set out to do this. Gi, Gs and Gq protein-mediated responses were assessed utilizing endogenous or heterologously expressed receptors in Chinese hamster ovary cells. UBO-QIC, at 1 μM, was an effective inhibitor of the Gq-mediated responses, but was inactive at Gi- and Gs-mediated responses. Gq/11 and G16 responses were additionally compared in HEL92.1.7 cells, showing inhibition of Gq/11 responses. However, UBO-QIC also appeared to inhibit G16. Further studies are required to establish its profile with respect to the different Gq-family proteins. Copyright © 2015 Elsevier Inc. All rights reserved.