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2rkp

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[[Image:2rkp.jpg|left|200px]]
[[Image:2rkp.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2rkp |SIZE=350|CAPTION= <scene name='initialview01'>2rkp</scene>, resolution 1.56&Aring;
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The line below this paragraph, containing "STRUCTURE_2rkp", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Cl+Binding+Site+For+Residue+A+336'>AC1</scene>, <scene name='pdbsite=AC2:Cl+Binding+Site+For+Residue+A+337'>AC2</scene>, <scene name='pdbsite=AC3:Cl+Binding+Site+For+Residue+A+338'>AC3</scene>, <scene name='pdbsite=AC4:Cl+Binding+Site+For+Residue+A+339'>AC4</scene>, <scene name='pdbsite=AC5:Cl+Binding+Site+For+Residue+A+340'>AC5</scene>, <scene name='pdbsite=AC6:Cl+Binding+Site+For+Residue+A+341'>AC6</scene>, <scene name='pdbsite=AC7:Cl+Binding+Site+For+Residue+A+342'>AC7</scene>, <scene name='pdbsite=AC8:Cl+Binding+Site+For+Residue+A+343'>AC8</scene>, <scene name='pdbsite=AC9:Cl+Binding+Site+For+Residue+A+344'>AC9</scene>, <scene name='pdbsite=BC1:Cl+Binding+Site+For+Residue+A+345'>BC1</scene>, <scene name='pdbsite=BC2:Cl+Binding+Site+For+Residue+A+346'>BC2</scene>, <scene name='pdbsite=BC3:Cl+Binding+Site+For+Residue+A+347'>BC3</scene>, <scene name='pdbsite=BC4:Cl+Binding+Site+For+Residue+A+348'>BC4</scene>, <scene name='pdbsite=BC5:Cl+Binding+Site+For+Residue+A+349'>BC5</scene>, <scene name='pdbsite=BC6:Cl+Binding+Site+For+Residue+A+350'>BC6</scene>, <scene name='pdbsite=BC7:Cl+Binding+Site+For+Residue+A+351'>BC7</scene>, <scene name='pdbsite=BC8:Rfz+Binding+Site+For+Residue+A+352'>BC8</scene> and <scene name='pdbsite=BC9:Rfz+Binding+Site+For+Residue+A+353'>BC9</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=RFZ:5,6-DICHLORO-1-BETA-D-RIBOFURANOSYL-1H-BENZIMIDAZOLE'>RFZ</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CSNK2A1 or CK2A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2rkp| PDB=2rkp | SCENE= }}
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|RELATEDENTRY=[[1pjk|1PJK]], [[1ymi|1YMI]], [[1lp4|1LP4]], [[1foq|1FOQ]], [[2pvr|2PVR]], [[1jwh|1JWH]], [[1j91|1J91]], [[1day|1DAY]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2rkp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2rkp OCA], [http://www.ebi.ac.uk/pdbsum/2rkp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2rkp RCSB]</span>
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}}
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'''Crystal structure of the catalytic subunit of human protein kinase CK2 with 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole'''
'''Crystal structure of the catalytic subunit of human protein kinase CK2 with 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole'''
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[[Category: Niefind, K.]]
[[Category: Niefind, K.]]
[[Category: Raaf, J.]]
[[Category: Raaf, J.]]
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[[Category: allosteric binding site]]
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[[Category: Allosteric binding site]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: drb]]
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[[Category: Drb]]
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[[Category: eukaryotic protein kinase fold]]
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[[Category: Eukaryotic protein kinase fold]]
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[[Category: human ck2alpha]]
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[[Category: Human ck2alpha]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: protein kinase ck2]]
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[[Category: Protein kinase ck2]]
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[[Category: protein kinase inhibitor complex]]
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[[Category: Protein kinase inhibitor complex]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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[[Category: wnt signaling pathway]]
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[[Category: Wnt signaling pathway]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 17:05:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:01:32 2008''
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Revision as of 14:06, 4 May 2008

Image:2rkp.jpg

Template:STRUCTURE 2rkp

Crystal structure of the catalytic subunit of human protein kinase CK2 with 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole


Overview

The Ser/Thr kinase CK2 (previously called casein kinase 2) is composed of two catalytic chains (CK2alpha) attached to a dimer of noncatalytic subunits (CK2beta). CK2 is involved in suppression of apoptosis, cell survival, and tumorigenesis. To investigate these activities and possibly affect them, selective CK2 inhibitors are required. An often-used CK2 inhibitor is 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB). In a complex structure with human CK2alpha, DRB binds to the canonical ATP cleft, but additionally it occupies an allosteric site that can be alternatively filled by glycerol. Inhibition kinetic studies corroborate the dual binding mode of the inhibitor. Structural comparisons reveal a surprising conformational plasticity of human CK2alpha around both DRB binding sites. After local rearrangement, the allosteric site serves as a CK2beta interface. This opens the potential to construct molecules interfering with the CK2alpha/CK2beta interaction.

About this Structure

2RKP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The CK2alpha/CK2beta Interface of Human Protein Kinase CK2 Harbors a Binding Pocket for Small Molecules., Raaf J, Brunstein E, Issinger OG, Niefind K, Chem Biol. 2008 Feb;15(2):111-7. PMID:18291315 Page seeded by OCA on Sun May 4 17:05:58 2008

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