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. 2019 Aug 28;14(9):2024–2034. doi: 10.1021/acschembio.9b00505

Figure 1.

Figure 1

Design and cellular activity of first generation SGK3 PROTACs. (A) Structure of compound 14H, previously published by Sanofi as an inhibitor of SGK3. (B) Starting material for SGK PROTACs. PROTACs were derived from SGK inhibitors 308-R or 290-R linked to either VH032 or pomalidomide to target the VHL or cereblon E3 ligases, respectively. (C) Structures of first generation SGK PROTACs. SGK and E3 ligase targeting motifs were joined by a 3xPEG linker to produce the PROTACs. (D) HEK293 cells were treated for 48 h with increasing concentrations of each PROTAC compound from 0.1 nM to 10 μM. Cell lysates were subjected to immunoblot analysis with the indicated antibodies, and SGK3 protein levels were quantified in Image Studio Lite software (Licor).