2uvx
From Proteopedia
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- | [[Image:2uvx.jpg|left|200px]]<br /><applet load="2uvx" size="350" color="white" frame="true" align="right" spinBox="true" | ||
- | caption="2uvx, resolution 2.00Å" /> | ||
- | '''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 7-AZAINDOLE'''<br /> | ||
- | == | + | ==Structure of PKA-PKB chimera complexed with 7-azaindole== |
- | + | <StructureSection load='2uvx' size='340' side='right'caption='[[2uvx]], [[Resolution|resolution]] 2.00Å' scene=''> | |
- | [[ | + | == Structural highlights == |
- | [[ | + | <table><tr><td colspan='2'>[[2uvx]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Bovin Bovin]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2UVX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2UVX FirstGlance]. <br> |
- | [[ | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GVH:1H-PYRROLO[2,3-B]PYRIDINE'>GVH</scene></td></tr> |
- | [[ | + | <tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr> |
- | [[ | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1cmk|1cmk]], [[1xh4|1xh4]], [[1xh5|1xh5]], [[1xh6|1xh6]], [[1xh7|1xh7]], [[1xh8|1xh8]], [[1xh9|1xh9]], [[1xha|1xha]], [[1ydr|1ydr]], [[2c1a|2c1a]], [[2c1b|2c1b]], [[2f7e|2f7e]], [[2gni|2gni]], [[2jds|2jds]], [[2jdt|2jdt]], [[2jdv|2jdv]], [[1kmu|1kmu]], [[1kmw|1kmw]], [[1q24|1q24]], [[1q61|1q61]], [[1q62|1q62]], [[1q8t|1q8t]], [[1q8u|1q8u]], [[1q8w|1q8w]], [[1smh|1smh]], [[1stc|1stc]], [[1sve|1sve]], [[1svg|1svg]], [[1svh|1svh]], [[1szm|1szm]], [[1veb|1veb]], [[1yds|1yds]], [[1ydt|1ydt]], [[2gfc|2gfc]], [[2gnf|2gnf]], [[2gng|2gng]], [[2gnh|2gnh]], [[2gnj|2gnj]], [[2gnl|2gnl]], [[2uvy|2uvy]], [[2uvz|2uvz]], [[2uw0|2uw0]]</div></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=2uvx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2uvx OCA], [https://pdbe.org/2uvx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2uvx RCSB], [https://www.ebi.ac.uk/pdbsum/2uvx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2uvx ProSAT]</span></td></tr> |
- | [[ | + | </table> |
- | [[ | + | == Function == |
- | [[ | + | [[https://www.uniprot.org/uniprot/IPKA_HUMAN IPKA_HUMAN]] Extremely potent competitive inhibitor of cAMP-dependent protein kinase activity, this protein interacts with the catalytic subunit of the enzyme after the cAMP-induced dissociation of its regulatory chains. |
- | [[ | + | == Evolutionary Conservation == |
- | [[ | + | [[Image:Consurf_key_small.gif|200px|right]] |
- | [[ | + | Check<jmol> |
- | [[ | + | <jmolCheckbox> |
- | [[ | + | <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/uv/2uvx_consurf.spt"</scriptWhenChecked> |
- | [[ | + | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> |
- | [[ | + | <text>to colour the structure by Evolutionary Conservation</text> |
- | [[ | + | </jmolCheckbox> |
- | [[ | + | </jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2uvx ConSurf]. |
- | [[ | + | <div style="clear:both"></div> |
- | [[ | + | <div style="background-color:#fffaf0;"> |
- | [[ | + | == Publication Abstract from PubMed == |
- | [[ | + | 6-phenylpurines were identified as novel, ATP-competitive inhibitors of protein kinase B (PKB/Akt) from a fragment-based screen and were rapidly progressed to potent compounds using iterative protein-ligand crystallography with a PKA-PKB chimeric protein. An elaborated lead compound showed cell growth inhibition and effects on cellular signaling pathways characteristic of PKB inhibition. |
- | [[ | + | |
- | [ | + | |
- | + | Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.,Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24. PMID:17451235<ref>PMID:17451235</ref> | |
+ | |||
+ | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
+ | </div> | ||
+ | <div class="pdbe-citations 2uvx" style="background-color:#fffaf0;"></div> | ||
+ | |||
+ | ==See Also== | ||
+ | *[[CAMP-dependent protein kinase 3D structures|CAMP-dependent protein kinase 3D structures]] | ||
+ | == References == | ||
+ | <references/> | ||
+ | __TOC__ | ||
+ | </StructureSection> | ||
+ | [[Category: Bovin]] | ||
+ | [[Category: Large Structures]] | ||
+ | [[Category: Aherne, G W]] | ||
+ | [[Category: Boyle, R G]] | ||
+ | [[Category: Collins, I]] | ||
+ | [[Category: Davies, T G]] | ||
+ | [[Category: Donald, A]] | ||
+ | [[Category: Garrett, M D]] | ||
+ | [[Category: Hunter, L J]] | ||
+ | [[Category: McHardy, T]] | ||
+ | [[Category: Rowlands, M G]] | ||
+ | [[Category: Atp- binding]] | ||
+ | [[Category: Camp]] | ||
+ | [[Category: Kinase]] | ||
+ | [[Category: Lipoprotein]] | ||
+ | [[Category: Myristate]] | ||
+ | [[Category: Nuclear protein]] | ||
+ | [[Category: Nucleotide-binding]] | ||
+ | [[Category: Phosphorylation]] | ||
+ | [[Category: Protein kinase inhibitor]] | ||
+ | [[Category: Serine/threonine-protein kinase]] | ||
+ | [[Category: Transferase]] | ||
+ | [[Category: Transferase-inhibitor complex]] | ||
+ | [[Category: Transferase/inhibitor]] |
Current revision
Structure of PKA-PKB chimera complexed with 7-azaindole
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Categories: Bovin | Large Structures | Aherne, G W | Boyle, R G | Collins, I | Davies, T G | Donald, A | Garrett, M D | Hunter, L J | McHardy, T | Rowlands, M G | Atp- binding | Camp | Kinase | Lipoprotein | Myristate | Nuclear protein | Nucleotide-binding | Phosphorylation | Protein kinase inhibitor | Serine/threonine-protein kinase | Transferase | Transferase-inhibitor complex | Transferase/inhibitor