Fig. 4: Discovery of FUT8 inhibitor FDW028. | Cell Death & Disease

Fig. 4: Discovery of FUT8 inhibitor FDW028.

From: FDW028, a novel FUT8 inhibitor, impels lysosomal proteolysis of B7-H3 via chaperone-mediated autophagy pathway and exhibits potent efficacy against metastatic colorectal cancer

Fig. 4

A Strategies for [1, 2, 4] triazolo [1,5-a] pyrimidin-7-ol skeleton discovery. B Docking prediction of FDW028 binding to FUT8. C Binding kinetics for FUT8 versus FDW028 obtained from GCI experiments. Sensograms are shown in multiple color with the respective fits in black, and include table summaries of the dissociation constant KD. D Protein thermal shift assay curves for FUT8 with 200 μM FDW028 at gradient temperatures from 39.0 to 59.0 °C (up), or with the indicated concentration of FDW028 at 51.9 °C [45]. E The immunoblots (up) and LC–MS/MS spectrum [45] of FUT8 that was pulled down by FDW028-biotin. The structure of FDW028-biotin is also shown.

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