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. 2015 Mar 19;6(12):10445–10459. doi: 10.18632/oncotarget.3398

Figure 5. Evidence that EGFR/HER2/HER3-targeted Compounds Can Function as Disulfide Bond Disrupting Agents (DDAs).

Figure 5

A. Proposed model for how DDAs disrupt disulfide bonds by inserting into them and potentially changing their connectivity (a and b). Should cyclization of the pharmacophore occur to form DTDO, reaction with free thiols or thiolates (c) may lead to incorporation of the pharmacophore into the protein. B, C. Mass spectra of reactions carried out between 10 mM RBF3 and 10 mM reduced (B) or oxidized (C) glutathione for 24 hours at 37°C, pH 7.0. D, E. Mass spectra of reactions carried out between 10 mM DTDO (D) or 10 mM RBF6 (E) and 10 mM reduced glutathione for 24 hours at 37°C, pH 7.0. Reactions between DTDO or RBF6 and oxidized glutathione did not lead to products and the related mass spectra are not shown (see SI).