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. Author manuscript; available in PMC: 2013 Nov 21.
Published in final edited form as: J Am Chem Soc. 2012 Nov 6;134(46):19017–19025. doi: 10.1021/ja306035v

Figure 4.

Figure 4

The STE kinase LOK adopts the DFG-out conformation. (A) Crystal structure of the catalytic domain of LOK bound to the type I inhibitor SU11274 (PBD 2j7t). The DGF-motif of LOK (shown in green) is in the active conformation. (B) Crystal structure of the LOK-inhibitor 1 complex. The DFG-motif of LOK (shown in green) adopts the DFG-out conformation when bound to inhibitor 1. Inhibitor 1 makes all of the characteristic contacts of type II inhibitors. (B) In vitro labeling of the purified catalytic domain of LOK with probe 4.