5jj2

Crystal structure of the central domain of human AKAP18 gamma/delta in complex with malonate

spinqualitylabelsall models 5jj2, resolution 1.25Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5jj2 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.25Å Ligands: MLI Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function AKA7G_HUMAN Probably targets cAMP-dependent protein kinase (PKA) to the cellular membrane or cytoskeletal structures. The membrane-associated form reduces epithelial sodium channel (ENaC) activity, whereas the free cytoplasmic form may negatively regulate ENaC channel feedback inhibition by intracellular sodium. Publication Abstract from PubMed A-kinase anchoring proteins (AKAPs) are a family of proteins that provide spatiotemporal resolution of protein kinase A (PKA) phosphorylation. In the myocardium, PKA and AKAP18gamma/delta are found in complex with sarcoendoplasmic reticulum Ca(2+)-ATPase 2 (SERCA2) and phospholamban (PLB). This macromolecular complex provides a means by which anchored PKA can dynamically regulate cytoplasmic Ca(2+) release and re-uptake. For this reason, AKAP18gamma/delta presents an interesting drug target with therapeutic potential in cardiovascular disease. The crystal structure of the central domain of human AKAP18gamma has been determined at the atomic resolution of 1.25 A. This first structure of human AKAP18gamma is trapped in a novel conformation by a malonate molecule bridging the important R-loop with the 2H phosphoesterase motif. Although the physiological substrate of AKAP18gamma is currently unknown, a potential proton wire deep in the central binding crevice has been indentified, leading to bulk solvent below the R-loop. Malonate complexed with AKAP18gamma at atomic resolution provides an excellent starting point for structure-guided drug design. Malonate in the nucleotide-binding site traps human AKAP18gamma/delta in a novel conformational state.,Bjerregaard-Andersen K, Ostensen E, Scott JD, Tasken K, Morth JP Acta Crystallogr F Struct Biol Commun. 2016 Aug;72(Pt 8):591-7. doi:, 10.1107/S2053230X16010189. Epub 2016 Jul 13. PMID:27487922 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also A-kinase anchor protein 3D structures

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