6fdz: Difference between revisions

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'''Unreleased structure'''


The entry 6fdz is ON HOLD  until Jun 27 2019
==Unc-51-Like Kinase 3 (ULK3) In Complex With Momelotinib==
 
<StructureSection load='6fdz' size='340' side='right' caption='[[6fdz]], [[Resolution|resolution]] 2.55&Aring;' scene=''>
Authors: Mathea, S., Salah, E., Moroglu, M., Scorah, A., Pike, A.C.W., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Huber, K., Knapp, S.
== Structural highlights ==
 
<table><tr><td colspan='2'>[[6fdz]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6FDZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6FDZ FirstGlance]. <br>
Description: Unc-51-Like Kinase 3 (ULK3) In Complex With Momelotinib
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=C87:Momelotinib'>C87</scene></td></tr>
[[Category: Unreleased Structures]]
<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>
[[Category: Moroglu, M]]
<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=6fdz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6fdz OCA], [http://pdbe.org/6fdz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6fdz RCSB], [http://www.ebi.ac.uk/pdbsum/6fdz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6fdz ProSAT]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/ULK3_HUMAN ULK3_HUMAN]] Serine/threonine protein kinase that acts as a regulator of Sonic hedgehog (SHH) signaling and autophagy. Acts as a negative regulator of SHH signaling in the absence of SHH ligand: interacts with SUFU, thereby inactivating the protein kinase activity and preventing phosphorylation of GLI proteins (GLI1, GLI2 and/or GLI3). Positively regulates SHH signaling in the presence of SHH: dissociates from SUFU, autophosphorylates and mediates phosphorylation of GLI2, activating it and promoting its nuclear translocation. Phosphorylates in vitro GLI2, as well as GLI1 and GLI3, although less efficiently. Also acts as a regulator of autophagy: following cellular senescence, able to induce autophagy.<ref>PMID:19279323</ref> <ref>PMID:19878745</ref> <ref>PMID:20643644</ref> 
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Arrowsmith, C H]]
[[Category: Bountra, C]]
[[Category: Delft, F von]]
[[Category: Edwards, A M]]
[[Category: Huber, K]]
[[Category: Knapp, S]]
[[Category: Knapp, S]]
[[Category: Huber, K]]
[[Category: Scorah, A]]
[[Category: Mathea, S]]
[[Category: Mathea, S]]
[[Category: Pike, A.C.W]]
[[Category: Moroglu, M]]
[[Category: Edwards, A.M]]
[[Category: Pike, A C.W]]
[[Category: Arrowsmith, C.H]]
[[Category: Salah, E]]
[[Category: Salah, E]]
[[Category: Von Delft, F]]
[[Category: Scorah, A]]
[[Category: Bountra, C]]
[[Category: Kinase inhibitor dfg-out]]
[[Category: Transferase]]

Latest revision as of 21:54, 1 August 2018

Unc-51-Like Kinase 3 (ULK3) In Complex With MomelotinibUnc-51-Like Kinase 3 (ULK3) In Complex With Momelotinib

Structural highlights

6fdz is a 1 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, PDBe, RCSB, PDBsum, ProSAT

Function

[ULK3_HUMAN] Serine/threonine protein kinase that acts as a regulator of Sonic hedgehog (SHH) signaling and autophagy. Acts as a negative regulator of SHH signaling in the absence of SHH ligand: interacts with SUFU, thereby inactivating the protein kinase activity and preventing phosphorylation of GLI proteins (GLI1, GLI2 and/or GLI3). Positively regulates SHH signaling in the presence of SHH: dissociates from SUFU, autophosphorylates and mediates phosphorylation of GLI2, activating it and promoting its nuclear translocation. Phosphorylates in vitro GLI2, as well as GLI1 and GLI3, although less efficiently. Also acts as a regulator of autophagy: following cellular senescence, able to induce autophagy.[1] [2] [3]

References

  1. ↑ Young AR, Narita M, Ferreira M, Kirschner K, Sadaie M, Darot JF, Tavare S, Arakawa S, Shimizu S, Watt FM, Narita M. Autophagy mediates the mitotic senescence transition. Genes Dev. 2009 Apr 1;23(7):798-803. doi: 10.1101/gad.519709. Epub 2009 Mar 11. PMID:19279323 doi:http://dx.doi.org/10.1101/gad.519709
  2. ↑ Maloverjan A, Piirsoo M, Michelson P, Kogerman P, Osterlund T. Identification of a novel serine/threonine kinase ULK3 as a positive regulator of Hedgehog pathway. Exp Cell Res. 2010 Feb 15;316(4):627-37. doi: 10.1016/j.yexcr.2009.10.018. Epub, 2009 Oct 21. PMID:19878745 doi:http://dx.doi.org/10.1016/j.yexcr.2009.10.018
  3. ↑ Maloverjan A, Piirsoo M, Kasak L, Peil L, Osterlund T, Kogerman P. Dual function of UNC-51-like kinase 3 (Ulk3) in the Sonic hedgehog signaling pathway. J Biol Chem. 2010 Sep 24;285(39):30079-90. doi: 10.1074/jbc.M110.133991. Epub, 2010 Jul 19. PMID:20643644 doi:http://dx.doi.org/10.1074/jbc.M110.133991

6fdz, resolution 2.55Å

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