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. Author manuscript; available in PMC: 2020 Mar 21.
Published in final edited form as: Cell Chem Biol. 2019 Jan 3;26(3):390–399.e5. doi: 10.1016/j.chembiol.2018.11.005

Figure 2: DDR1 binds type I inhibitors in the DFG-Asp-out conformation.

Figure 2:

A) Co-crystal structure of DDR1·VX-680 [PDB-entry: 6BRJ] with activation loop (blue), phosphate binding P-loop (red), helix αC (orange). B) The co-crystal structure of DDR1·dasatinib [PDB-entry: 6BSD] with regulatory elements colored as in A. C) Comparison of type I (top, VX-680/dasatinib) and type II (bottom, imatinib/ponatinib) inhibitors binding to Abl (green, right column) and DDR1 kinase (blue, left column). Only the protein surrounding the DFG-motif is shown for clarity. D) Comparison of Φ dihedral angle for Asp747 in DDR1 (blue) and Abl (green) bound to the type I and type II inhibitors in panel C. See also Figure S3.