A homogeneous time-resolved fluorescence screen to identify SIRT2 deacetylase and defatty-acylase inhibitors
Fig 6
Enhanced affinity of 2 for the SIRT2—decanoyl-peptide complex compared to SIRT2 alone.
2 was used to displace the fluorescent ligand 1-aminoanthracene from SIRT2’s hydrophobic tunnel which resulted in a reduction of 1-aminoanthracene fluorescence. The concentration of 1-aminoanthracene was 100 nM, the SIRT2 concentration was 4 μM, and when added, the concentration of decanoyl-H4K16 peptide was 10 μM. The IC50 values were used to calculate Kd values of 68 μM for the interaction of 2 with SIRT2 and 3 μM for the interaction of 2 with the SIRT2—decanoyl-peptide complex [12]. The Kd of 68 μM for its SIRT2 interaction was also reported in Fig 5.