Colin A. Flaveny

TL;DR: Mechanistic studies show that SR1 acts by antagonizing the aryl hydrocarbon receptor (AHR) and AHR modulation as a means to induce ex vivo HSC expansion should facilitate the clinical use of HSC therapy.

TL;DR: KA is a potent AHR endogenous ligand that can induce IL6 production and xenobiotic metabolism in cells at physiologically relevant concentrations and it is established that the carboxylic acid group is required for significant agonist activity.

TL;DR: Indoxyl 3-sulfate represents the first identified relatively high potency endogenous AHR ligand that plays a key role in human disease progression and may contribute to toxicity observed in kidney dialysis patients and thus represent a possible therapeutic target.

TL;DR: In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression and suggest that LXR inverse agonists may be an effective cancer treatment approach.

TL;DR: It is noteworthy that competitive ligand-binding assays revealed that, compared with the mAHR, the hAHR has a higher relative affinity for certain compounds, including indirubin, which may imply that there may be a significant degree of structural divergence between mA HR and hA HR ligands and highlights the importance of the HAHR transgenic mouse as a model to study the AHR in vivo.