5ajq: Difference between revisions

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'''Unreleased structure'''
==Human LOK (STK10) in complex with Bosutinib==
 
<StructureSection load='5ajq' size='340' side='right' caption='[[5ajq]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
The entry 5ajq is ON HOLD
== Structural highlights ==
 
<table><tr><td colspan='2'>[[5ajq]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5AJQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AJQ FirstGlance]. <br>
Authors: Elkins, J.M., Salah, E., Krojer, T., Kopec, J., Bountra, C., Edwards, A.M., Knapp, S.
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DB8:4-[(2,4-DICHLORO-5-METHOXYPHENYL)AMINO]-6-METHOXY-7-[3-(4-METHYLPIPERAZIN-1-YL)PROPOXY]QUINOLINE-3-CARBONITRILE'>DB8</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
 
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>
Description: Human LOK (STK10) in complex with Bosutinib
<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=5ajq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ajq OCA], [http://www.rcsb.org/pdb/explore.do?structureId=5ajq RCSB], [http://www.ebi.ac.uk/pdbsum/5ajq PDBsum]</span></td></tr>
[[Category: Unreleased Structures]]
</table>
[[Category: Elkins, J.M]]
== Disease ==
[[http://www.uniprot.org/uniprot/STK10_HUMAN STK10_HUMAN]] The disease may be caused by mutations affecting the gene represented in this entry.<ref>PMID:16175573</ref> 
== Function ==
[[http://www.uniprot.org/uniprot/STK10_HUMAN STK10_HUMAN]] Serine/threonine-protein kinase involved in regulation of lymphocyte migration. Phosphorylates MSN, and possibly PLK1. Involved in regulation of lymphocyte migration by mediating phosphorylation of ERM proteins such as MSN. Acts as a negative regulator of MAP3K1/MEKK1. May also act as a cell cycle regulator by acting as a polo kinase kinase: mediates phosphorylation of PLK1 in vitro; however such data require additional evidences in vivo.<ref>PMID:11903060</ref> <ref>PMID:12639966</ref> <ref>PMID:19255442</ref> 
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Bountra, C]]
[[Category: Edwards, A M]]
[[Category: Elkins, J M]]
[[Category: Knapp, S]]
[[Category: Knapp, S]]
[[Category: Kopec, J]]
[[Category: Krojer, T]]
[[Category: Krojer, T]]
[[Category: Bountra, C]]
[[Category: Kopec, J]]
[[Category: Edwards, A.M]]
[[Category: Salah, E]]
[[Category: Salah, E]]
[[Category: Transferase]]

Revision as of 15:03, 11 March 2015

Human LOK (STK10) in complex with BosutinibHuman LOK (STK10) in complex with Bosutinib

Structural highlights

5ajq is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:, ,
Activity:Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Resources:FirstGlance, OCA, RCSB, PDBsum

Disease

[STK10_HUMAN] The disease may be caused by mutations affecting the gene represented in this entry.[1]

Function

[STK10_HUMAN] Serine/threonine-protein kinase involved in regulation of lymphocyte migration. Phosphorylates MSN, and possibly PLK1. Involved in regulation of lymphocyte migration by mediating phosphorylation of ERM proteins such as MSN. Acts as a negative regulator of MAP3K1/MEKK1. May also act as a cell cycle regulator by acting as a polo kinase kinase: mediates phosphorylation of PLK1 in vitro; however such data require additional evidences in vivo.[2] [3] [4]

References

  1. ↑ Bignell G, Smith R, Hunter C, Stephens P, Davies H, Greenman C, Teague J, Butler A, Edkins S, Stevens C, O'Meara S, Parker A, Avis T, Barthorpe S, Brackenbury L, Buck G, Clements J, Cole J, Dicks E, Edwards K, Forbes S, Gorton M, Gray K, Halliday K, Harrison R, Hills K, Hinton J, Jones D, Kosmidou V, Laman R, Lugg R, Menzies A, Perry J, Petty R, Raine K, Shepherd R, Small A, Solomon H, Stephens Y, Tofts C, Varian J, Webb A, West S, Widaa S, Yates A, Gillis AJ, Stoop HJ, van Gurp RJ, Oosterhuis JW, Looijenga LH, Futreal PA, Wooster R, Stratton MR. Sequence analysis of the protein kinase gene family in human testicular germ-cell tumors of adolescents and adults. Genes Chromosomes Cancer. 2006 Jan;45(1):42-6. PMID:16175573 doi:http://dx.doi.org/10.1002/gcc.20265
  2. ↑ Tao L, Wadsworth S, Mercer J, Mueller C, Lynn K, Siekierka J, August A. Opposing roles of serine/threonine kinases MEKK1 and LOK in regulating the CD28 responsive element in T-cells. Biochem J. 2002 Apr 1;363(Pt 1):175-82. PMID:11903060
  3. ↑ Walter SA, Cutler RE Jr, Martinez R, Gishizky M, Hill RJ. Stk10, a new member of the polo-like kinase kinase family highly expressed in hematopoietic tissue. J Biol Chem. 2003 May 16;278(20):18221-8. Epub 2003 Mar 13. PMID:12639966 doi:http://dx.doi.org/10.1074/jbc.M212556200
  4. ↑ Belkina NV, Liu Y, Hao JJ, Karasuyama H, Shaw S. LOK is a major ERM kinase in resting lymphocytes and regulates cytoskeletal rearrangement through ERM phosphorylation. Proc Natl Acad Sci U S A. 2009 Mar 24;106(12):4707-12. doi:, 10.1073/pnas.0805963106. Epub 2009 Mar 2. PMID:19255442 doi:http://dx.doi.org/10.1073/pnas.0805963106

5ajq, resolution 2.20Å

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