2vgp | pdb_00002vgp
| |||||||||||||
| 2vgp, resolution 1.70Å | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sites: | AC1 and AC2 | ||||||||||||
| Ligands: | AD6, TPO | ||||||||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||||||||
| Domains: | S_TKc, S_TKc, INCENP_ARK-bind | ||||||||||||
| Related: | 2BFX, 2BFY, 2VGO
| ||||||||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
CRYSTAL STRUCTURE OF AURORA B KINASE IN COMPLEX WITH A AMINOTHIAZOLE INHIBITOR
Overview
Aurora family kinases regulate important events during mitosis including centrosome maturation and separation, mitotic spindle assembly, and chromosome segregation. Misregulation of Aurora kinases due to genetic amplification and protein overexpression results in aneuploidy and may contribute to tumorigenesis. Here we report the discovery of new small molecule aminothiazole inhibitors of Aurora kinases with exceptional kinase selectivity and report a 1.7 A cocrystal structure with the Aurora B:INCENP complex from Xenopus laevis. The compounds recapitulate the hallmarks of Aurora kinase inhibition, including decreased histone H3 serine 10 phosphorylation, failure to complete cytokinesis, and endoreduplication.
About this Structure
2VGP is a Protein complex structure of sequences from Xenopus laevis. Full crystallographic information is available from OCA.
Reference
Discovery of selective aminothiazole aurora kinase inhibitors., Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS, ACS Chem Biol. 2008 Mar 20;3(3):180-92. Epub 2008 Feb 29. PMID:18307303
Page seeded by OCA on Mon Mar 31 05:12:02 2008
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- Non-specific serine/threonine protein kinase
- Protein complex
- Xenopus laevis
- Andersen, C B.
- Chang, J W.
- Gray, N S.
- Lee, C.
- Liu, Y.
- Musacchio, A.
- Nallan, L.
- Sessa, F.
- Villa, F.
- Wan, Y.
- Aminothiazole
- Atp-binding
- Aurora b
- Cancer
- Cell cycle
- Cell division
- Centromere
- Coiled coil
- Incenp
- Kinase
- Magnesium
- Metal-binding
- Microtubule
- Mitosis
- Nucleotide-binding
- Nucleus
- Phosphorylation
- Serine/threonine-protein kinase
- Transferase
