Figure 1.
Crystal structures of EphA3 in complex with inhibitors that preserve the DFG-in conformation. (Top) Type I inhibitors 1 (carbon atoms in yellow, PDB code 4GK3), 4 (salmon, 4P4C), 5 (blue, 4P5Q), and 7 (orange, 4TWO). (Bottom) Type I1/2 inhibitors 2 (green, 4GK2), 3 (cyan, 4GK4), and 8 (magenta, 4G2F). The side chains of the DFG motif Phe765 and the Glu670 of the C helix are also shown (carbon atoms in gray). All nitrogen and oxygen atoms are in blue and red, respectively. The Cα atoms of EphA3 were used for the structural superposition in all figures.