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. Author manuscript; available in PMC: 2018 Feb 16.
Published in final edited form as: Mol Cell. 2017 Feb 16;65(4):644–658.e5. doi: 10.1016/j.molcel.2017.01.014

Figure 7. The activity cycle of PTP1B.

Figure 7

The PTP1B catalytic cycle and its allosteric control (free/open, outer circle; inhibitor bound/closed, inner circle).

(A→B) Binding of the active site inhibitor TCS401 pushes the W179 aromatic side chain towards P185 (P185 makes a CH/π switch from F269 to W179).

(C→D) This allows for the closing of the WPD loop.

(E→F) The resulting ‘F191 push’ causes helix α3 to rotate.

(G→H) This allows S190 to hydrogen bond with S187, extending and stabilizing helix α3.

(I→J) This allows N193 to interact with Y152 and E295.