Orthogonal kinase inhibitors

Active Inhibitor-insensitive Kinase Mutants (Orthogonal Protein Kinases)... 

Fig. 8.16 The PP1 analogue that is an orthogonal ligand inhibitor specific for the F88G variant of the cyclin-dependent kinase Cdc28.

A large number of examples for the orthogonal dipolar C-F—C=0 interactions have been found in the CSD and PDB [101], For example, Figure 1.13b illustrates a rather unique double interaction, that is, C-F—(C=0)2, in the inhibitor-enzyme complex of 26 with p38 MAP kinase, wherein the fluorine atom of the 4-fluorophenyl moiety of 26 interacts with the amide carbonyl carbons of Leul04 and Vall05 with equal distance of 3.1 A [102],... 

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