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Figure 6.
DFG-out conformation in PYK2. A, conformational change for
the DFG motif upon binding of BIRB796. DFG-in motif in Apo
structure is shown in purple and the DFG-out conformation in
green. B, superposition of the structures of the PYK2: BIRB796
complex (green) from p38: BIRB796 complex (orange) showing
significant differences represented by arrows. C, stereoview
showing the DFG-out binding sites of Imatinib from Abl (yellow),
Sorafenib from B-RAF (gray), and BIRB796 from PYK2 (cyan) with
corresponding gatekeeper residues. D, β-turn conformation in
the hinge region with hydrogen bonds in dashes; Apo structure
(pink), PYK2:BIRB796 complex (cyan), and PYK2:PF-4618433 (green).
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