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. Author manuscript; available in PMC: 2023 Jan 26.
Published in final edited form as: J Am Chem Soc. 2022 Jan 18;144(3):1152–1157. doi: 10.1021/jacs.1c12702

Figure 4.

Figure 4.

Reversible covalent inhibition of SrtA. (a) SrtA structure with docked W7 (PDB: 1t2w). The peptide’s termini and the proximal lysine residues are labeled with the lysine ε-amines colored blue. K173 (in light blue shade) was found to be the conjugation site for P5. (b) Chemical structure of W7 and the warheads for its modification. (c) IC50 values of various peptides measured through competition against W7-F. C# represent iodoacetamide-alkylated cysteines. ¥P5 was N-acetylated to prevent RMR1 conjugation with the N-terminus. (d, e) SrtA binding kinetics of P3 and P5 recorded via a competition assay using W7-F as a fluorescence reporter.