Figure 1 | Scientific Reports

Figure 1

From: Small molecule inhibitors of the mitochondrial ClpXP protease possess cytostatic potential and re-sensitize chemo-resistant cancers

Figure 1

Small molecule 334 is a promising candidate for inhibition of the ClpXP complex. (a) The chemical structures of the small molecules 319, 334 and 339 inhibiting the ClpXP complex. For the chemical structure of all molecules tested for inhibition see also Supplementary Fig. S1 online. (b) Small molecules with activity towards the bacterial SaClpXP complex were tested for their inhibitory potential against the HsClpXP isoform. The ClpXP enzyme activity was assessed by fluorescence recording of cleaved FITC-casein conjugates (n = 3). (c) Promising candidates 319, 334 and 339 were additionally tested for inhibition of the HsClpP peptidase activity. Enzymatic activity of HsClpP was measured by monitoring the cleavage of the fluorogenic substrate Ac-Ala-hArg-2-Aoc-ACC (n = 4).

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