4j7b

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Crystal structure of polo-like kinase 1Crystal structure of polo-like kinase 1

Structural highlights

4j7b is a 6 chain structure with sequence from Danio rerio and Drosophila melanogaster. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.3Å
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

Q6DRK7_DANRE

Publication Abstract from PubMed

Polo-like kinase 1 (PLK1) is a master regulator of mitosis and is considered a potential drug target for cancer therapy. PLK1 is characterized by an N-terminal kinase domain (KD) and a C-terminal Polo-box domain (PBD). The KD and PBD are mutually inhibited, but the molecular mechanisms of the autoinhibition remain unclear. Here we report the 2.3-A crystal structure of the complex of the Danio rerio KD and PBD together with a PBD-binding motif of Drosophila melanogaster microtubule-associated protein 205 (Map205(PBM)). The structure reveals that the PBD binds and rigidifies the hinge region of the KD in a distinct conformation from that of the phosphopeptide-bound PBD. This structure provides a framework for understanding the autoinhibitory mechanisms of PLK1 and also sheds light on the activation mechanisms of PLK1 by phosphorylation or phosphopeptide binding.

Structural basis for the inhibition of Polo-like kinase 1.,Xu J, Shen C, Wang T, Quan J Nat Struct Mol Biol. 2013 Sep;20(9):1047-53. doi: 10.1038/nsmb.2623. Epub 2013, Jul 28. PMID:23893132[1]

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

References

  1. Xu J, Shen C, Wang T, Quan J. Structural basis for the inhibition of Polo-like kinase 1. Nat Struct Mol Biol. 2013 Sep;20(9):1047-53. doi: 10.1038/nsmb.2623. Epub 2013, Jul 28. PMID:23893132 doi:10.1038/nsmb.2623

4j7b, resolution 2.30Å

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OCA