4yc4
From Proteopedia
Crystal structure of phosphatidyl inositol 4-kinase II alpha in complex with nucleotide analog
Structural highlights
Function[P4K2A_HUMAN] Together with PI4K2B and the type III PI4Ks (PIK4CA and PIK4CB) it contributes to the overall PI4-kinase activity of the cell. The phosphorylation of phosphatidylinositol (PI) to PI4P is the first committed step in the generation of phosphatidylinositol 4,5-bisphosphate (PIP2), a precursor of the second messenger inositol 1,4,5-trisphosphate (InsP3). Contributes to the production of InsP3 in stimulated cells (By similarity). This lipid kinase is the major phosphatidylinositol 4-phosphate (PI4P) producer in the Golgi apparatus, it generates more than 50% of this molecule which is essential for the identity of the organelle, protein sorting and membrane trafficking. Publication Abstract from PubMedPhosphatidylinositol 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 IIbeta and PI4K IIalpha. In this study, two crystal structures are presented: the structure of human PI4K IIbeta and the structure of PI4K IIalpha containing a nucleoside analogue. The former, a complex with ATP, is the first high-resolution (1.9 A) 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. The high-resolution crystal structure of phosphatidylinositol 4-kinase IIbeta and the crystal structure of phosphatidylinositol 4-kinase IIalpha containing a nucleoside analogue provide a structural basis for isoform-specific inhibitor design.,Klima M, Baumlova A, Chalupska D, Hrebabecky H, Dejmek M, Nencka R, Boura E Acta Crystallogr D Biol Crystallogr. 2015 Jul 1;71(Pt 7):1555-63. doi:, 10.1107/S1399004715009505. Epub 2015 Jun 30. PMID:26143926[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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Categories: Boura, E | Klima, M | Complex | Inhibitor | Kinase | Transferase
