4b6l: Difference between revisions

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'''Unreleased structure'''
{{STRUCTURE_4b6l|  PDB=4b6l  |  SCENE=  }}
===Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design===


The entry 4b6l is ON HOLD until Paper Publication
==Function==
[[http://www.uniprot.org/uniprot/PLK3_HUMAN PLK3_HUMAN]] Serine/threonine-protein kinase involved in cell cycle regulation, response to stress and Golgi disassembly. Polo-like kinases act by binding and phosphorylating proteins are that already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates ATF2, BCL2L1, CDC25A, CDC25C, CHEK2, HIF1A, JUN, p53/TP53, p73/TP73, PTEN, TOP2A and VRK1. Involved in cell cycle regulation: required for entry into S phase and cytokinesis. Phosphorylates BCL2L1, leading to regulate the G2 checkpoint and progression to cytokinesis during mitosis. Plays a key role in response to stress: rapidly activated upon stress stimulation, such as ionizing radiation, reactive oxygen species (ROS), hyperosmotic stress, UV irradiation and hypoxia. Involved in DNA damage response and G1/S transition checkpoint by phosphorylating CDC25A, p53/TP53 and p73/TP73. Phosphorylates p53/TP53 in response to reactive oxygen species (ROS), thereby promoting p53/TP53-mediated apoptosis. Phosphorylates CHEK2 in response to DNA damage, promoting the G2/M transition checkpoint. Phosphorylates the transcription factor p73/TP73 in response to DNA damage, leading to inhibit p73/TP73-mediated transcriptional activation and pro-apoptotic functions. Phosphorylates HIF1A and JUN is response to hypoxia. Phosphorylates ATF2 following hyperosmotic stress in corneal epithelium. Also involved in Golgi disassembly during the cell cycle: part of a MEK1/MAP2K1-dependent pathway that induces Golgi fragmentation during mitosis by mediating phosphorylation of VRK1. May participate in endomitotic cell cycle, a form of mitosis in which both karyokinesis and cytokinesis are interrupted and is a hallmark of megakaryocyte differentiation, via its interaction with CIB1.<ref>PMID:12242661</ref> <ref>PMID:9353331</ref> <ref>PMID:10557092</ref> <ref>PMID:11156373</ref> <ref>PMID:11447225</ref> <ref>PMID:11551930</ref> <ref>PMID:11971976</ref> <ref>PMID:14980500</ref> <ref>PMID:14968113</ref> <ref>PMID:15021912</ref> <ref>PMID:16478733</ref> <ref>PMID:16481012</ref> <ref>PMID:17804415</ref> <ref>PMID:17264206</ref> <ref>PMID:18062778</ref> <ref>PMID:18650425</ref> <ref>PMID:19490146</ref> <ref>PMID:19103756</ref> <ref>PMID:20889502</ref> <ref>PMID:20940307</ref> <ref>PMID:21098032</ref> <ref>PMID:21840391</ref> <ref>PMID:21376736</ref> <ref>PMID:21264284</ref>  


Authors: Brown, K., Charrier, J.D., Durrant, S., Griffiths, M., Hudson, C., Kay, D., Knegtel, R., ODonnell, M., Pierard, F., Twin, H., Weber, P., Young, S.
==About this Structure==
[[4b6l]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4B6L OCA].  


Description: Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design
==Reference==
<references group="xtra"/><references/>
[[Category: Homo sapiens]]
[[Category: Polo kinase]]
[[Category: Brown, K.]]
[[Category: Charrier, J D.]]
[[Category: Durrant, S.]]
[[Category: Griffiths, M.]]
[[Category: Hudson, C.]]
[[Category: Kay, D.]]
[[Category: Knegtel, R.]]
[[Category: ODonnell, M.]]
[[Category: Pierard, F.]]
[[Category: Twin, H.]]
[[Category: Weber, P.]]
[[Category: Young, S.]]
[[Category: Kinase inhibitor]]
[[Category: Transferase]]
[[Category: Water-mediated h-bond]]
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