3bw5
From Proteopedia
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|PDB= 3bw5 |SIZE=350|CAPTION= <scene name='initialview01'>3bw5</scene>, resolution 1.66Å | |PDB= 3bw5 |SIZE=350|CAPTION= <scene name='initialview01'>3bw5</scene>, resolution 1.66Å | ||
|SITE= <scene name='pdbsite=AC1:Cl+Binding+Site+For+Residue+A+336'>AC1</scene>, <scene name='pdbsite=AC2:Anp+Binding+Site+For+Residue+A+340'>AC2</scene> and <scene name='pdbsite=AC3:Gol+Binding+Site+For+Residue+A+341'>AC3</scene> | |SITE= <scene name='pdbsite=AC1:Cl+Binding+Site+For+Residue+A+336'>AC1</scene>, <scene name='pdbsite=AC2:Anp+Binding+Site+For+Residue+A+340'>AC2</scene> and <scene name='pdbsite=AC3:Gol+Binding+Site+For+Residue+A+341'>AC3</scene> | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=ANP:PHOSPHOAMINOPHOSPHONIC+ACID-ADENYLATE+ESTER'>ANP</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene> |
| - | |ACTIVITY= [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] | + | |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> |
|GENE= csnk2a1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= csnk2a1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[2rkp|2RKP]], [[1day|1DAY]], [[1j91|1J91]], [[1jwh|1JWH]], [[2pvr|2PVR]], [[1lp4|1LP4]], [[1pjk|1PJK]], [[3bqc|3BQC]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3bw5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3bw5 OCA], [http://www.ebi.ac.uk/pdbsum/3bw5 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3bw5 RCSB]</span> | ||
}} | }} | ||
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[[Category: Raaf, J.]] | [[Category: Raaf, J.]] | ||
[[Category: Yde, C W.]] | [[Category: Yde, C W.]] | ||
| - | [[Category: ANP]] | ||
| - | [[Category: CL]] | ||
| - | [[Category: GOL]] | ||
[[Category: atp-binding]] | [[Category: atp-binding]] | ||
[[Category: casein kinase 2]] | [[Category: casein kinase 2]] | ||
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[[Category: wnt signaling pathway]] | [[Category: wnt signaling pathway]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:29:25 2008'' |
Revision as of 02:29, 31 March 2008
| |||||||
| , resolution 1.66Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | , and | ||||||
| Ligands: | , , | ||||||
| Gene: | csnk2a1 (Homo sapiens) | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Related: | 2RKP, 1DAY, 1J91, 1JWH, 2PVR, 1LP4, 1PJK, 3BQC
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal structure of a mutant of human protein kinase CK2alpha with altered cosubstrate specificity
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
3BW5 is a Single protein structure of sequence from Homo sapiens. This structure supersedes the now removed PDB entry 1YMI. 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 Mon Mar 31 05:29:25 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Ermakova, I. | Issinger, O G. | Niefind, K. | Raaf, J. | Yde, C W. | Atp-binding | Casein kinase 2 | Casein kinase ii | Nucleotide-binding | Protein kinase ck2 | Serine/threonine-protein kinase | Transferase | Wnt signaling pathway
