2rkp | pdb_00002rkp
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| 2rkp, resolution 1.56Å | |||||||||||||
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| Sites: | AC1, AC2, AC3, AC4, AC5, AC6, AC7, AC8, AC9, BC1, BC2, BC3, BC4, BC5, BC6, BC7, BC8 and BC9 | ||||||||||||
| Ligands: | CL, RFZ | ||||||||||||
| Gene: | CSNK2A1 or CK2A1 (Homo sapiens) | ||||||||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||||||||
| Related: | 1PJK, 1YMI, 1LP4, 1FOQ, 2PVR, 1JWH, 1J91, 1DAY
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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 Mon Mar 31 05:01:32 2008
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- Homo sapiens
- Non-specific serine/threonine protein kinase
- Single protein
- Issinger, O G.
- Niefind, K.
- Raaf, J.
- Allosteric binding site
- Atp-binding
- Drb
- Eukaryotic protein kinase fold
- Human ck2alpha
- Nucleotide-binding
- Protein kinase ck2
- Protein kinase inhibitor complex
- Serine/threonine-protein kinase
- Transferase
- Wnt signaling pathway
