Title | Computational analysis of phosphopeptide binding to the polo-box domain of the mitotic kinase PLK1 using molecular dynamics simulation. |
Publication Type | Journal Article |
Year of Publication | 2010 |
Authors | Huggins DJ, McKenzie GJ, Robinson DD, Narváez AJ, Hardwick B, Roberts-Thomson M, Venkitaraman AR, Grant GH, Payne MC |
Journal | PLoS Comput Biol |
Volume | 6 |
Issue | 8 |
Date Published | 2010 Aug 12 |
ISSN | 1553-7358 |
Keywords | Binding Sites, cdc25 Phosphatases, Cell Cycle Proteins, Humans, Molecular Dynamics Simulation, Phosphopeptides, Phosphorylation, Phosphothreonine, Protein Binding, Protein Interaction Domains and Motifs, Protein-Serine-Threonine Kinases, Proto-Oncogene Proteins, Substrate Specificity |
Abstract | The Polo-Like Kinase 1 (PLK1) acts as a central regulator of mitosis and is over-expressed in a wide range of human tumours where high levels of expression correlate with a poor prognosis. PLK1 comprises two structural elements, a kinase domain and a polo-box domain (PBD). The PBD binds phosphorylated substrates to control substrate phosphorylation by the kinase domain. Although the PBD preferentially binds to phosphopeptides, it has a relatively broad sequence specificity in comparison with other phosphopeptide binding domains. We analysed the molecular determinants of recognition by performing molecular dynamics simulations of the PBD with one of its natural substrates, CDC25c. Predicted binding free energies were calculated using a molecular mechanics, Poisson-Boltzmann surface area approach. We calculated the per-residue contributions to the binding free energy change, showing that the phosphothreonine residue and the mainchain account for the vast majority of the interaction energy. This explains the very broad sequence specificity with respect to other sidechain residues. Finally, we considered the key role of bridging water molecules at the binding interface. We employed inhomogeneous fluid solvation theory to consider the free energy of water molecules on the protein surface with respect to bulk water molecules. Such an analysis highlights binding hotspots created by elimination of water molecules from hydrophobic surfaces. It also predicts that a number of water molecules are stabilized by the presence of the charged phosphate group, and that this will have a significant effect on the binding affinity. Our findings suggest a molecular rationale for the promiscuous binding of the PBD and highlight a role for bridging water molecules at the interface. We expect that this method of analysis will be very useful for probing other protein surfaces to identify binding hotspots for natural binding partners and small molecule inhibitors. |
DOI | 10.1371/journal.pcbi.1000880 |
Alternate Journal | PLoS Comput Biol |
PubMed ID | 20711360 |
PubMed Central ID | PMC2920843 |
Grant List | MC_U105359877 / / Medical Research Council / United Kingdom G9900064 / / Medical Research Council / United Kingdom G0600332 / / Medical Research Council / United Kingdom RG55039 / / Medical Research Council / United Kingdom G0700651 / / Medical Research Council / United Kingdom |