Thierry Da Cunha

TL;DR: The effect of glycyrrhetinic acid and GA-derivatives towards 11beta-hydroxysteroid dehydrogenase (11beta-HSD) was investigated and single crystal X-ray diffraction data of selected substances are reported and discussed.

TL;DR: 3D-structure modeling provides an explanation for the differences in the selectivity and activity of the GA derivatives investigated, and should prove useful as mechanistic tools for further anti-inflammatory and anti-cancer in vitro and in vivo studies.

TL;DR: The results reveal that 11β-HSD1 is responsible for 7-oxoLCA reduction in humans, providing a further link between hepatic glucocorticoid activation and bile acid metabolism, and suggest the need for animal and clinical studies to explore whether inhibition of 11 β- HSD1 to reduce cortisol levels would also lead to an accumulation of 7- oxo LCA, thereby potentially affecting bile acids-mediated functions.

TL;DR: A pharmacophore model based on the crystal structure of the GA-derivative carbenoxolone in complex with human 11beta-HSD1 is provided, providing an explanation for the differences in the activities of 18alpha-GA and 18beta-GA.

TL;DR: It was established that the main factor governing the relatively poor precision of submicrometer methods in general and inherently, is their low sampling volume and the corresponding large extrapolation factors for calculating final results.