FIGURE

Fig. 4

ID

ZDB-FIG-240729-84

Publication

Dernovšek et al., 2024 - Exploration and optimisation of structure-activity relationships of new triazole-based C-terminal Hsp90 inhibitors towards in vivo anticancer potency

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Fig. 4

Biochemical evaluation of Hsp90 CTD binding using TR-FRET. Residual activities of Hsp90β (A) and Hsp90α (B) CTD when triazole-based inhibitors were applied at 100 µM concentration: compounds C, 5a, 5f, 5p, 5r, 5s, 5t, 5u, 5v, 5w and 5x from Library A are shown in red, compounds 8g, 10g, 10f, and 10i from Library B along with novobiocin at 1000 µM and positive control are presented in blue. The bars represent mean values with SD of at least three replicates. Statistical significance was calculated using one sample t-test (*p<0.05, **p<0.01, ***p<0.001); C) Schematic representation of the mechanism of the TR-FRET assay in which the C-terminal Hsp90 inhibitor prevents the interaction of cyclophilin D and Hsp90 CTD; D) Dose-response curves for compound 5x in the luciferase refolding assay in two biological repetitions performed in triplicates.

Expression Data

Expression Detail

Antibody Labeling

Phenotype Data

Phenotype Detail

Acknowledgments

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