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Simple, non-macrocyclic inhibitors bind FKBPl2 as tightly as FK506 and potently inhibit the peptidyl prolyl isomerase activity of that enzyme. The structure of one of these in complex with FKBPI2 is presented.
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The structure of FKBPl2 is reported for the first time in its unliganded form, and in complex with 18 inhibitors. Analysis of these structures suggests that FKBP12 is locally flexible.