research papers
Phosphatidylinositol 4-phosphate (PI4P) is the most abundant monophosphoinositide in eukaryotic cells. Humans have four phosphatidylinositol 4-kinases (PI4Ks) that synthesize PI4P, among which are PI4K IIβ and PI4K IIα. In this study, two crystal structures are presented: the structure of human PI4K IIβ and the structure of PI4K IIα containing a nucleoside analogue. The former, a complex with ATP, is the first high-resolution (1.9 Å) structure of a PI4K. These structures reveal new details such as high conformational heterogeneity of the lateral hydrophobic pocket of the C-lobe and together provide a structural basis for isoform-specific inhibitor design.
Supporting information
Portable Document Format (PDF) file https://doi.org/10.1107/S1399004715009505/dz5370sup1.pdf |
PDB references: phosphatidylinositol 4-kinase IIβ, 4wtv; phosphatidylinositol 4-kinase IIα, complex with nucleotide analogue, 4yc4