G-protein inhibition profile of the reported Gq/11 inhibitor UBO-QIC
JP Kukkonen - Biochemical and biophysical research communications, 2016 - Elsevier
JP Kukkonen
Biochemical and biophysical research communications, 2016•ElsevierAbstract UBO-QIC (FR900359) is the only currently available G q/11 protein inhibitor.
However, its characterization has not been published, and we thus set out to do this. G i, G s
and G q 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 G q-mediated responses, but was inactive at G i-and G s-mediated
responses. G q/11 and G 16 responses were additionally compared in HEL92. 1.7 cells …
However, its characterization has not been published, and we thus set out to do this. G i, G s
and G q 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 G q-mediated responses, but was inactive at G i-and G s-mediated
responses. G q/11 and G 16 responses were additionally compared in HEL92. 1.7 cells …
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.
Elsevier
