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

Document Type

Article

Publication Date

9-15-2017

Publication Title

European journal of pharmacology

Abstract

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/metabolism; Animals; Anti-Inflammatory Agents/pharmacology; Isoxazoles/pharmacology; Lipopolysaccharides/pharmacology; Macrophages/cytology/drug effects; Mice; Phosphoproteins/metabolism; Proteomics; RAW 264.7 Cells; STAT3 Transcription Factor/metabolism; Signal Transduction/drug effects; Anti-inflammatory; Lps; Macrophage; Mass spectrometry; Phosphoproteomics; UTL-5g

PubMed ID

28576409

Volume

811

First Page

66

Last Page

73

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