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. 2020 Sep 13;12(9):2613. doi: 10.3390/cancers12092613

Figure 3.

Figure 3

Identification of POLA2 as a new Erlotinib binding protein. (a) DARTS assay validating the Erlotinib-POLA2 interaction. POLA2 protein was stabilized in the presence of pronase after Erlotinib treatment in H1299 cells. Pronase treatment was applied for 20 min with Erlotinib in a dose-dependent manner; (b) CETSA validation of the erlotinib-POLA2 interaction. POLA2 protein was stabilized under heat treatment (61 °C for 5 min) and different Erlotinib treatments in a dose-dependent manner; (c) In silico docking analysis of the interaction between Erlotinib and POLA2 (human N-terminal POLA2, RCSB PDB ID: 2KEB). Erlotinib binds to the TYR34-surrounded POLA2 pocket in the most stable position; binding motifs are depicted as several high-affinity interactions between Erlotinib and the POLA2 pocket. Ligands are shown as gray sticks in charge receptor surfaces. Bonds are shown as dashed lines color-coded as in (c).