Fig. 1: Illustration of TMP-eDHFR PROTAC system and chemical approach. | Nature Communications

Fig. 1: Illustration of TMP-eDHFR PROTAC system and chemical approach.

From: Regulation of eDHFR-tagged proteins with trimethoprim PROTACs

Fig. 1

A The protein of interest (POI) is fused to the N- or C-terminus of eDHFR. The fusion protein is expressed in the absence of TMP PROTAC and is degraded in the presence of the regulating ligand via the proteasome. B Synthesis of TMP-pomalidomide PROTACs. (i) HBr, 90 °C, 20 min, 1 M NaOH; (ii) t-BuOK, DMSO, 2 h/Cs2CO3, DMF, 70 °C, 12 h; (iii) K2CO3, MeOH, H2O, 70 °C, 12 h; (iv) DIPEA, DMF, 90 °C, 12 h; (v) TFA, DCM, room temperature (rt), overnight; (vi) Cs2CO3, iodomethane, DMF; (vii) PyAOP, DIPEA, DMF, 30 min, rt.

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