Assay Method Information

Assay Name:  Enzyme Inhibition Assay
Description:  Enzyme activity was determined by monitoring the quantity of sialylated disaccharide product produced over time at 348 nm by RP-HPLC (Supelco Discovery HS C18, 5 um, 4.6 mmx25 cm). Retention time of the product was 20.38 minutes.The described sixteen synthetic analogues showed decreased IC50 s compared to lithocholic acid (Table 1). The terminal alcohol 7 and its derivative 8 displayed a 5 to 17-fold decrease over lithocholic acid, suggesting that a carboxylic acid group is important for promoting, affinity. This was further confirmed by using peptide coupling to extend the terminal carboxylic acid; the inhibitor), properties of compounds 9 and 10 can be restored completely compared to those of 7-8. To determine the importance of the 3-hydroxyl position of lithocholic acid, the inhibition of alpha -2,3-ST activity by compound 11, which has a ketone moiety in place of a hydroxyl group, was evaluated.
Affinity data for this assay
 

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