Kukkonen Jyrki P
Biochemistry and Cell Biology, Department of Veterinary Biosciences, POB 66, FIN-00014, University of Helsinki, Finland.
Biochem Biophys Res Commun. 2016 Jan 1;469(1):101-107. doi: 10.1016/j.bbrc.2015.11.078. Epub 2015 Nov 22.
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.
UBO-QIC（FR900359）是目前唯一可用的Gq/11蛋白抑制剂。然而，其特性尚未发表，因此我们着手进行此项研究。利用中国仓鼠卵巢细胞中的内源性或异源表达受体评估Gi、Gs和Gq蛋白介导的反应。1μM的UBO-QIC是Gq介导反应的有效抑制剂，但对Gi和Gs介导的反应无活性。此外，在HEL92.1.7细胞中比较了Gq/11和G16反应，结果显示Gq/11反应受到抑制。然而，UBO-QIC似乎也能抑制G16。需要进一步研究以确定其针对不同Gq家族蛋白的特性。
