Gue1654
OXE-R biased antagonist / Gue1654 is a biased antagonist for the oxoeicosanoid receptor 1 (OXE-R, GPR170)1, the receptor for 5-Oxo-ETE, a proinflammatory eicosanoid2. It selectively inhibits Gβγ but not Gαi signaling upon activation of the Gαi-βγ heterotrimer by OXE-R.1,3 Gue1654 alleviated coronary artery ligation-induced ischemic myocardial injury in a mouse model.4
Biochemicals & reagents
397290-30-1
1 Blatermann et al. (2012), A biased ligand for OXE-R uncouples Gα and Gßγ signaling within a heterotrimer; Nat. Chem. Biol., 8 631 2 Powell and Rokach (2013), The eosinophil chemoattractant 5-oxo-ETE and the OXE receptor; Prog. Lipid Res., 52 651 3 Konya et al. (2014), A biased non-Gαi OXE-R antagonist demonstrates that Gαi protein subunit is not directly involved in neutrophil, eosinophil, and monocyte activation by 5-oxo-ETE; J. Immunol., 192 4774 4 Lai et al. (2021), Oxoeicosanoid receptor inhibition alleviates acute myocardial infarction though activation of BCAT1; Basic Res. Cardiol., 116 3
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TARGET: GPCR -- PATHWAY: Lipid signaling -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer; InflammationIschemia