Phosphoproteome and transcription factor activity profiling identify actions of the anti-inflammatory agent UTL-5g in LPS stimulated RAW 2647 cells including disrupting actin remodeling and STAT-3 activation
Carruthers NJ, Stemmer PM, Chen B, Valeriote F, Gao X, Guatam SC, and Shaw J. Phosphoproteome and transcription factor activity profiling identify actions of the anti-inflammatory agent UTL-5g in LPS stimulated RAW 264.7 cells including disrupting actin remodeling and STAT-3 activation. Eur J Pharmacol 2017; 811:66-73.
European journal of pharmacology
UTL-5g is a novel small-molecule TNF-alpha modulator. It reduces cisplatin-induced side effects by protecting kidney, liver, and platelets, thereby increasing tolerance for cisplatin. UTL-5g also reduces radiation-induced acute liver toxicity. The mechanism of action for UTL-5g is not clear at the present time. A phosphoproteomic analysis to a depth of 4943 phosphopeptides and a luminescence-based transcription factor activity assay were used to provide complementary analyses of signaling events that were disrupted by UTL-5g in RAW 264.7 cells. Transcriptional activity downstream of the interferon gamma, IL-6, type 1 Interferon, TGF-β, PKC/Ca
Medical Subject Headings
Actins; Animals; Anti-Inflammatory Agents; Isoxazoles; Lipopolysaccharides; Macrophages; Mice; Phosphoproteins; Proteomics; RAW 264.7 Cells; STAT3 Transcription Factor; Signal Transduction