5jj2
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==Crystal structure of the central domain of human AKAP18 gamma/delta in complex with malonate== | ==Crystal structure of the central domain of human AKAP18 gamma/delta in complex with malonate== | ||
| - | <StructureSection load='5jj2' size='340' side='right' caption='[[5jj2]], [[Resolution|resolution]] 1.25Å' scene=''> | + | <StructureSection load='5jj2' size='340' side='right'caption='[[5jj2]], [[Resolution|resolution]] 1.25Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5jj2]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5JJ2 OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[5jj2]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5JJ2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5JJ2 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MLI:MALONATE+ION'>MLI</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.25Å</td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MLI:MALONATE+ION'>MLI</scene></td></tr> |
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5jj2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5jj2 OCA], [https://pdbe.org/5jj2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5jj2 RCSB], [https://www.ebi.ac.uk/pdbsum/5jj2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5jj2 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/AKA7G_HUMAN 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.<ref>PMID:10613906</ref> <ref>PMID:17244820</ref> |
| + | <div style="background-color:#fffaf0;"> | ||
| + | == 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. | ||
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| + | 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<ref>PMID:27487922</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 5jj2" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[A-kinase anchor protein 3D structures|A-kinase anchor protein 3D structures]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Bjerregaard-Andersen K]] |
| - | + | [[Category: Morth JP]] | |
| - | + | [[Category: Ostensen E]] | |
| - | [[Category: | + | [[Category: Scott JD]] |
| - | [[Category: | + | [[Category: Tasken K]] |
| - | [[Category: | + | |
| - | [[Category: | + | |
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Current revision
Crystal structure of the central domain of human AKAP18 gamma/delta in complex with malonate
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