5j0a
From Proteopedia
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== Function == | == Function == | ||
[https://www.uniprot.org/uniprot/TOPK_HUMAN TOPK_HUMAN] Phosphorylates MAP kinase p38. Seems to be active only in mitosis. May also play a role in the activation of lymphoid cells. When phosphorylated, forms a complex with TP53, leading to TP53 destabilization and attenuation of G2/M checkpoint during doxorubicin-induced DNA damage.<ref>PMID:10781613</ref> <ref>PMID:17482142</ref> | [https://www.uniprot.org/uniprot/TOPK_HUMAN TOPK_HUMAN] Phosphorylates MAP kinase p38. Seems to be active only in mitosis. May also play a role in the activation of lymphoid cells. When phosphorylated, forms a complex with TP53, leading to TP53 destabilization and attenuation of G2/M checkpoint during doxorubicin-induced DNA damage.<ref>PMID:10781613</ref> <ref>PMID:17482142</ref> | ||
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- | == Publication Abstract from PubMed == | ||
- | The overexpression of PDZ-binding kinase/T-LAK cell-originated protein kinase (PBK/TOPK) has been associated with hematologic tumors, breast cancer and various other cancers. However, the three-dimensional structure of PBK has not been solved. In this study, we determined the crystal structure of human PBK, which has two phospho-mimicking mutations T9E and T198E. The structural data indicated that PBK may assemble into an inactive dimer in alkaline conditions. Analytical size-exclusion chromatography and analytical ultracentrifugation confirmed that PBK exists in a conformational transition between dimers and monomers at different pH conditions. Co-IP and kinase assays suggested that the active state of PBK is a monomer and does not form a dimer even under alkaline conditions. These results showed that the conformational transition of PBK is important for its kinase activity regulation. Collectively, our observations may provide a novel starting point for structure-based functional studies. | ||
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- | The crystal structure of an inactive dimer of PDZ-binding kinase.,Dong C, Tang X, Xie Y, Zou Q, Yang X, Zhou H Biochem Biophys Res Commun. 2016 Aug 5;476(4):586-93. doi:, 10.1016/j.bbrc.2016.05.166. Epub 2016 Jun 1. PMID:27262437<ref>PMID:27262437</ref> | ||
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- | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
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- | <div class="pdbe-citations 5j0a" style="background-color:#fffaf0;"></div> | ||
== References == | == References == | ||
<references/> | <references/> |
Current revision
Crystal structure of PDZ-binding kinase
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Categories: Homo sapiens | Large Structures | Yang X | Zhou H | Zou QW