Table 1. Peptide numbering, sequence, inhibition constants, and binding energy as determined by fluorescence polarization (FP). The variable residues at the p+3 position are highlighted in bold. IC50 values were obtained from competitive binding experiments, converted to Ki according to the Coleska-Wang equation42, and ΔG calculated from the relationship, ΔG = RT ln Ki. Each value represents an average of 4 separate experiments.
# | Peptide Sequence | Ki (μM) | ΔG (kcal·mol−1) |
---|---|---|---|
1 | pYTPEP | 1.3 ± 0.6 | −7.95 ± 0.21 |
2 | pYTPAP | 18.1 ± 5.7 | −6.53 ± 0.22 |
3 | pYTPPP | 5.0 ± 2.2 | −7.32 ± 0.30 |