title: G-protein inhibition profile of the reported Gq/11 inhibitor UBO-QIC.
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.
authors.affiliation: Biochemistry and Cell Biology, Department of Veterinary Biosciences, POB 66, FIN-00014, University of Helsinki, Finland. Electronic address: jyrki.kukkonen@helsinki.fi.
authors.forename: Jyrki P
authors.initials: JP
authors.lastname: Kukkonen
mesh_terms: D000818:Animals; D016466:CHO Cells; D003412:Cricetulus; D047630:Depsipeptides / Q000008:administration & dosage* / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D043802:GTP-Binding Protein alpha Subunits, Gq-G11 / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D047630:Depsipeptides; C000607068:FR900359; D043802:GTP-Binding Protein alpha Subunits, Gq-G11
keywords: Adenylyl cyclase; G(i); G(q); G(s); Heterotrimeric G-protein; Phospholipase C