4b6l

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
{{STRUCTURE_4b6l| PDB=4b6l | SCENE= }}
+
==Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design==
-
===Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design===
+
<StructureSection load='4b6l' size='340' side='right' caption='[[4b6l]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[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]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4B6L FirstGlance]. <br>
 +
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=9ZP:4-[[(4R)-5-CYCLOPENTYL-4-ETHYL-3A,4-DIHYDRO-3H-[1,2,4]TRIAZOLO[4,3-F]PTERIDIN-7-YL]AMINO]-N-CYCLOPROPYL-3-METHOXY-BENZAMIDE'>9ZP</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
 +
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Polo_kinase Polo kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.21 2.7.11.21] </span></td></tr>
 +
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4b6l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4b6l OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4b6l RCSB], [http://www.ebi.ac.uk/pdbsum/4b6l PDBsum]</span></td></tr>
 +
</table>
-
==Function==
+
==See Also==
-
[[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>
+
*[[Serine/threonine protein kinase|Serine/threonine protein kinase]]
-
 
+
__TOC__
-
==About this Structure==
+
</StructureSection>
-
[[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].
+
-
 
+
-
==Reference==
+
-
<references group="xtra"/><references/>
+
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Polo kinase]]
[[Category: Polo kinase]]
-
[[Category: Brown, K.]]
+
[[Category: Brown, K]]
-
[[Category: Charrier, J D.]]
+
[[Category: Charrier, J D]]
-
[[Category: Durrant, S.]]
+
[[Category: Durrant, S]]
-
[[Category: Griffiths, M.]]
+
[[Category: Griffiths, M]]
-
[[Category: Hudson, C.]]
+
[[Category: Hudson, C]]
-
[[Category: Kay, D.]]
+
[[Category: Kay, D]]
-
[[Category: Knegtel, R.]]
+
[[Category: Knegtel, R]]
-
[[Category: ODonnell, M.]]
+
[[Category: ODonnell, M]]
-
[[Category: Pierard, F.]]
+
[[Category: Pierard, F]]
-
[[Category: Twin, H.]]
+
[[Category: Twin, H]]
-
[[Category: Weber, P.]]
+
[[Category: Weber, P]]
-
[[Category: Young, S.]]
+
[[Category: Young, S]]
[[Category: Kinase inhibitor]]
[[Category: Kinase inhibitor]]
[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Water-mediated h-bond]]
[[Category: Water-mediated h-bond]]

Revision as of 09:58, 21 December 2014

Discovery of Oral Polo-Like Kinase (PLK) Inhibitors with Enhanced Selectivity Profile using Residue Targeted Drug Design

4b6l, resolution 1.90Å

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4b6l"
Personal tools