View source for 4usf


==Human SLK with SB-440719==
<StructureSection load='4usf' size='340' side='right'caption='[[4usf]], [[Resolution|resolution]] 1.75&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4usf]] 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=4USF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4USF FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.75&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6UI:4-[4-(6-METHOXYNAPHTHALEN-2-YL)-1H-IMIDAZOL-5-YL]PYRIDINE'>6UI</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=4usf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4usf OCA], [https://pdbe.org/4usf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4usf RCSB], [https://www.ebi.ac.uk/pdbsum/4usf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4usf ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/SLK_HUMAN SLK_HUMAN] Mediates apoptosis and actin stress fiber dissolution.
<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&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 4usf" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Bountra C]]
[[Category: Edwards AM]]
[[Category: Elkins JM]]
[[Category: Knapp S]]
[[Category: Salah E]]
[[Category: Szklarz M]]
[[Category: Von Delft F]]