4use
From Proteopedia
(Difference between revisions)
| (3 intermediate revisions not shown.) | |||
| Line 1: | Line 1: | ||
| + | |||
==Human STK10 (LOK) with SB-633825== | ==Human STK10 (LOK) with SB-633825== | ||
| - | <StructureSection load='4use' size='340' side='right' caption='[[4use]], [[Resolution|resolution]] 2.65Å' scene=''> | + | <StructureSection load='4use' size='340' side='right'caption='[[4use]], [[Resolution|resolution]] 2.65Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4use]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4USE OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[4use]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4USE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4USE FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=R09:4-{5-(6-METHOXYNAPHTHALEN-2-YL)-1-METHYL-2-[2-METHYL-4-(METHYLSULFONYL)PHENYL]-1H-IMIDAZOL-4-YL}PYRIDINE'>R09</scene | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=R09:4-{5-(6-METHOXYNAPHTHALEN-2-YL)-1-METHYL-2-[2-METHYL-4-(METHYLSULFONYL)PHENYL]-1H-IMIDAZOL-4-YL}PYRIDINE'>R09</scene></td></tr> |
| - | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4use FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4use OCA], [https://pdbe.org/4use PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4use RCSB], [https://www.ebi.ac.uk/pdbsum/4use PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4use ProSAT]</span></td></tr> | |
| - | + | ||
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Disease == | == Disease == | ||
| - | [ | + | [https://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 == | == Function == | ||
| - | [ | + | [https://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> |
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Despite the success of protein kinase inhibitors as approved therapeutics, drug discovery has focused on a small subset of kinase targets. Here we provide a thorough characterization of the Published Kinase Inhibitor Set (PKIS), a set of 367 small-molecule ATP-competitive kinase inhibitors that was recently made freely available with the aim of expanding research in this field and as an experiment in open-source target validation. We screen the set in activity assays with 224 recombinant kinases and 24 G protein-coupled receptors and in cellular assays of cancer cell proliferation and angiogenesis. We identify chemical starting points for designing new chemical probes of orphan kinases and illustrate the utility of these leads by developing a selective inhibitor for the previously untargeted kinases LOK and SLK. Our cellular screens reveal compounds that modulate cancer cell growth and angiogenesis in vitro. These reagents and associated data illustrate an efficient way forward to increasing understanding of the historically untargeted kinome. | ||
| + | |||
| + | Comprehensive characterization of the Published Kinase Inhibitor Set.,Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Muller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ Nat Biotechnol. 2015 Oct 26. doi: 10.1038/nbt.3374. PMID:26501955<ref>PMID:26501955</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 4use" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Bountra | + | [[Category: Large Structures]] |
| - | [[Category: Canning | + | [[Category: Bountra C]] |
| - | [[Category: Edwards | + | [[Category: Canning P]] |
| - | [[Category: Elkins | + | [[Category: Edwards AM]] |
| - | [[Category: Knapp | + | [[Category: Elkins JM]] |
| - | [[Category: Raynor | + | [[Category: Knapp S]] |
| - | [[Category: Salah | + | [[Category: Raynor J]] |
| - | [[Category: Szklarz | + | [[Category: Salah E]] |
| - | [[Category: | + | [[Category: Szklarz M]] |
| - | + | [[Category: Von Delft F]] | |
Current revision
Human STK10 (LOK) with SB-633825
| |||||||||||
Categories: Homo sapiens | Large Structures | Bountra C | Canning P | Edwards AM | Elkins JM | Knapp S | Raynor J | Salah E | Szklarz M | Von Delft F
