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. 2021 Dec 31;12(6):2859–2868. doi: 10.1016/j.apsb.2021.12.017

Figure 2.

Figure 2

The rational design of NAMPT-specific proteolysis targeting chimeras (PROTACs). (A) The action mode of PROTACs via the ubiquitin–proteasome system (UPS). (B) The expected action of PROTACs on tumor cells and the tumor environment. (C) The chemical structure of MS7 and its predicted binding mode to NAMPT (PDB ID: 2GVJ). (D) The linkers of NAMPT-specific PROTACs. (E) Time-dependent NAMPT degradation. CT26 cells were treated with A7 (1 μmol/L) at different timepoints. (F) Dose-dependent degradation of NAMPT. A2780, HCT-116 or CT26 cells were treated with A7 at gradient concentrations (0, 0.01, 0.05, 0.2, 1, and 5 μmol/L) for 24 h.