2uvz: Difference between revisions

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<StructureSection load='2uvz' size='340' side='right'caption='[[2uvz]], [[Resolution|resolution]] 1.94&Aring;' scene=''>
<StructureSection load='2uvz' size='340' side='right'caption='[[2uvz]], [[Resolution|resolution]] 1.94&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[2uvz]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Bovin Bovin]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2UVZ OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2UVZ FirstGlance]. <br>
<table><tr><td colspan='2'>[[2uvz]] 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=2UVZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2UVZ FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GVJ:(S)-1-PHENYL-1-[4-(9H-PURIN-6-YL)PHENYL]METHANAMINE'>GVJ</scene></td></tr>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GVJ:(S)-1-PHENYL-1-[4-(9H-PURIN-6-YL)PHENYL]METHANAMINE'>GVJ</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='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">[[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]], [[2uvx|2uvx]], [[2uvy|2uvy]], [[2uw0|2uw0]]</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]], [[2uvx|2uvx]], [[2uvy|2uvy]], [[2uw0|2uw0]]</div></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2uvz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2uvz OCA], [http://pdbe.org/2uvz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2uvz RCSB], [http://www.ebi.ac.uk/pdbsum/2uvz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2uvz ProSAT]</span></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=2uvz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2uvz OCA], [https://pdbe.org/2uvz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2uvz RCSB], [https://www.ebi.ac.uk/pdbsum/2uvz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2uvz ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://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.  
[[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 ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]

Revision as of 15:31, 23 March 2022

Structure of PKA-PKB chimera complexed with C-Phenyl-C-(4-(9H-purin-6- yl)-phenyl)-methylamineStructure of PKA-PKB chimera complexed with C-Phenyl-C-(4-(9H-purin-6- yl)-phenyl)-methylamine

Structural highlights

2uvz is a 2 chain structure with sequence from Bovin. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
NonStd Res:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[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

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

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[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

See Also

References

  1. ↑ Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I. Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design. J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24. PMID:17451235 doi:10.1021/jm0700924

2uvz, resolution 1.94Å

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