Lara Dötsch, Caitlin Davies, Elisabeth Hennes, Julia Schönfeld, Adarsh Kumar, Celine Da Cruz Lopes Guita, Johanna H M Ehrler, Kerstin Hiesinger, Sasikala Thavam, Petra Janning, Sonja Sievers, Stefan Knapp, Ewgenij Proschak, Slava Ziegler, Herbert Waldmann
Disease-related phenotypic assays enable unbiased discovery of novel bioactive small molecules and may provide novel insights into physiological systems and unprecedented molecular modes of action (MMOA). Herein, we report the identification and characterization of epoxykynin, a potent inhibitor of the soluble epoxide hydrolase (sEH). Epoxykynin was discovered by means of a cellular assay monitoring modulation of kynurenine (Kyn) levels in BxPC-3 cells upon stimulation with the cytokine interferon-γ (IFN-γ) and subsequent target identification employing affinity-based chemical proteomics...
March 12, 2024: Journal of Medicinal Chemistry