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![[Figure 5]](chr5007fig5mag.jpg)
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Figure 5
Binding mode of BI 2536 in the ATP-binding site of PLK1K225D/K226A (SER approach) and in PLK1WT in complex with the DARPin. (a) Overall view of the complex of PLK1K225D/K226A (grey ribbon) and BI 2536 (in stick representation with C atoms in orange; PDB entry 9r1x). (b) 2Fo − Fc density map contoured at 1.3σ, with Cys133 in the hinge region and the gatekeeper residue Leu130 shown in stick representation. Hydrogen bonds are shown as dotted yellow lines. (c) Overall view of PLK1WT (grey ribbon representation), the DARPin (blue ribbon representation) and BI 2536 (stick representation, C atoms in green; PDB entry 9r8c). Heterodimer 2 (chains B and C) is shown of the two dimers in the asymmetric unit. (d) 2Fo − Fc density map contoured at 1.3σ, with PLK1 residues Cys133 (hinge) and Leu130 (gatekeeper) and DARPin residues Val78 and Met111 (in contact with the ligand) shown in stick representation. (e) Overlay of BI 2536 from both approaches, obtained by superimposition of the protein chains (chain A of the PLK1K225D/K226A structure and chain B of the DARPin structure). |
![[Figure 5]](chr5007fig5.jpg)
 | STRUCTURAL BIOLOGY |
ISSN: 2059-7983
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