5v3q

Human GSTO1-1 complexed with ML175

spinqualitylabelsall models 5v3q, resolution 2.25Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5v3q is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.25Å Ligands: MLX, SO4 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function GSTO1_HUMAN Exhibits glutathione-dependent thiol transferase and dehydroascorbate reductase activities. Has S-(phenacyl)glutathione reductase activity. Has also glutathione S-transferase activity. Participates in the biotransformation of inorganic arsenic and reduces monomethylarsonic acid (MMA) and dimethylarsonic acid. Publication Abstract from PubMed Glutathione transferase Omega 1 (GSTO1-1) is an atypical GST reported to play a pro-inflammatory role in response to LPS. Here we show that genetic knockout of Gsto1 alters the response of mice to three distinct inflammatory disease models. GSTO1-1 deficiency ameliorates the inflammatory response stimulated by LPS and attenuates the inflammatory impact of a high fat diet on glucose tolerance and insulin resistance. In contrast, GSTO1-1 deficient mice show a more severe inflammatory response and increased escape of bacteria from the colon into the lymphatic system in a dextran sodium sulfate mediated model of inflammatory bowel disease. These responses are similar to those of TLR4 and MyD88 deficient mice in these models and confirm that GSTO1-1 is critical for a TLR4-like pro-inflammatory response in vivo. In wild-type mice, we show that a small molecule inhibitor that covalently binds in the active site of GSTO1-1 can be used to ameliorate the inflammatory response to LPS. Our findings demonstrate the potential therapeutic utility of GSTO1-1 inhibitors in the modulation of inflammation and suggest their possible application in the treatment of a range of inflammatory conditions. GSTO1-1 plays a pro-inflammatory role in models of inflammation, colitis and obesity.,Menon D, Innes A, Oakley AJ, Dahlstrom JE, Jensen LM, Brustle A, Tummala P, Rooke M, Casarotto MG, Baell JB, Nguyen N, Xie Y, Cuellar M, Strasser J, Dahlin JL, Walters MA, Burgio G, O'Neill LAJ, Board PG Sci Rep. 2017 Dec 19;7(1):17832. doi: 10.1038/s41598-017-17861-6. PMID:29259211 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Glutathione S-transferase 3D structures

Proteopedia Page Contributors and Editors (what is this?)

OCA