Figure 2: Pharmacologic–phylogenetic relationship of iPGM macrocyclic peptide inhibitor. | Nature Communications

Figure 2: Pharmacologic–phylogenetic relationship of iPGM macrocyclic peptide inhibitor.

From: Macrocycle peptides delineate locked-open inhibition mechanism for microorganism phosphoglycerate mutases

Figure 2

(a) Structure of the Ce-2 macrocycle obtained from affinity selection showing truncation to give Ce-2d and position of Cys14Ser substitution. Note the thioether bond (yellow), D-tyrosine (blue), and thiol of Cys14 (light red). (b) IC50 dependence of Ce-2 on C. elegans iPGM enzyme concentration (50 pM to 1 μM), grey region indicated concentration range for PGMs used in initial inhibitory activity profiling obtained in Table 1. (c) Concentration-response curves for characterization of Ce-2d on the iPGM orthologues and dPGM isozymes. (d) Phylogenetic tree constructed for amino-acid sequence alignments of seven species orthologues and isozymes of PGM. Percentage bootstrap values based on 1,000 replicates are indicated at branch nodes. (e) Concentration-response curves for characterization of Ce-2S on the iPGM orthologues and dPGM isozymes. All data determined from the enzyme-coupled bioluminescent assay; PGM concentrations as indicated in Table 1. Plots are representatives from individual experiments (N=3); error bars are standard deviations values of technical replicates.

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