Fig. 1: Kinetic parameters on Caspase-2 versus Caspase-3 of P2-modified VDVAD pentapeptides derivatives.
From: Genuine selective caspase-2 inhibition with new irreversible small peptidomimetics
a Structures of reversible Caspase-2/3 inhibitors. Ac-VDVAD-CHO is a non-selective canonical pentapeptide Caspase-2/3 inhibitor, Ac-DEVD-CHO is a canonical tetrapeptide Caspase-3 inhibitor. c33, k33, q33, and h33 are VDVAD derivatives where the P2 Alanine residue was replaced by a bulky substituent to decrease activity against Caspase-3. b–e) Potent competitive inhibition of Caspase-2 by q33 (b, c) and h33 (d, e). Lineweaver-Burk plots of Casp2 inhibition with q33 (b) and h33 (d) are shown together with the relationship between the slopes of lines in Lineweaver–Burk plot analyses and the concentration of q33 (c) and h33 (e) inhibitors. f IC50, Ki values and Casp3/Casp2 selectivity ratio of reversible P2-modified VDVAD derivatives. Data points on the graphs represent the mean ± SD and calculated Ki values represent mean ± standard error (SE) from three independent experiments.
