mProX™ Human OXER1 Stable Cell Line

Panagiotopoulos AA, et al. "Mining the ZINC database of natural products for specific, testosterone-like, ." Steroids, 2023.
The receptor OXER1 has been found to have a significant role in inflammation, as it is responsible for chemotactic responses in white blood cells to the oxidized metabolite 5-oxo-ETE. Recently, the authors have identified OXER1 (GPR170) as a receptor for androgens in prostate and breast cancer cells. It has been observed that testosterone, through OXER1, induces calcium release and apoptosis, while also decreasing cancer cell migration. These effects are counteracted by 5-oxo-ETE. By mining the ZINC15 database, using QSAR, the authors have identified potential natural compounds that can mimic testosterone's actions and inhibit the tumor-promoting effects of 5-oxo-ETE. Four compounds with G(alphabetagamma) activity and seven with G(betagamma)-specific OXER1 interaction were discovered. Through bioinformatics analysis, the binding, ADMET (absorption, distribution, metabolism, excretion and toxicity) properties, and potential interaction with other receptors and enzymes were studied. Two compounds, ZINC04017374 and ZINC08589130, were purchased and tested in vitro, confirming their OXER1 G(betagamma) and G(alphabetagamma) activity, respectively. This methodology provides valuable insights into the mechanism of OXER1-mediated actions and can aid in designing new anti-inflammatory and anti-cancer agents. Furthermore, it has potential for identifying specific agonists/antagonists of other G protein-coupled receptors (GPCRs).
Pubmed: 37696380   DOI: 10.1016/j.steroids.2023.109309

Maus KD, et al. "Skewing cPLA(2)alpha activity toward oxoeicosanoid production promotes neutrophil N2 ." Science signaling, 2023.
The study analyzed the role of eicosanoids, which are bioactive lipids that recruit immune cells, in neutrophil polarization and function. To do so, the researchers investigated the effect of ceramide 1-phosphate (C1P), which interacts with the enzyme responsible for eicosanoid production, on neutrophil behavior. To examine this further, knockin mice expressing a cPLA(2) mutant without the C1P binding site were used. These mice showed increased and sustained neutrophil infiltration during the inflammatory phase of wound healing and sepsis, leading to improved wound healing and reduced susceptibility to sepsis. This was due to an increase in proresolution N2-type neutrophils and a decrease in proinflammatory N1-type neutrophils. The study concluded that C1P binding suppresses neutrophil N2 polarization, negatively impacting wound healing and response to sepsis.
Pubmed: 37433004   DOI: 10.1126/scisignal.add6527