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Figure 7.
Figure 7. The allosteric-bound conformation is similar to
conformations of PTP1B with the WPD loop in the open
conformation. (a) Overlay of 16 structures of PTP1B with the
WPD loop in the open conformation (black), along with PTP1B
bound to compound 2 (spheres, protein in magenta), and the
closed conformation (green, PDB entry 1PTY). Alignment shows
that the allosteric-bound conformation is similar to many open
conformations. (b) Allosteric inhibitor binds to the naturally
occurring open conformation (E[o]) of PTP1B and inhibits
activity by blocking closure of the WPD loop. Compound cannot
bind to the closed conformation.
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