Fig. 3: Coordination of the phosphorylated tyrosine and the CMGC insert region in HIPKs and DYRKs.
From: Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation
a In HIPK2, DYRK1A, DYRK2, and DYRK3 the phosphorylated tyrosine residue of the activation loop forms salt bridges with the arginines of the R(Y/F)YR motif. In HIPK3 instead, pY359 interacts with R431 of the CMGC insert region. b Variations of the β-hairpin loop conformation in the CMGC insert region. Protein structures shown in this figure are HIPK2 (6P5S, palegreen), HIPK3 (7O7I, blue/green), DYRK1A (2VX3, magenta), DYRK2 (3K2L, yellow), and DYRK3 (5Y86, salmon).
