4ff8: Difference between revisions
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==Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)== | |||
<StructureSection load='4ff8' size='340' side='right' caption='[[4ff8]], [[Resolution|resolution]] 2.40Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4ff8]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FF8 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3qup|3qup]], [[4feq|4feq]]</td></tr> | |||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])</td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ff8 PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity. | |||
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.,Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J 3rd, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ Bioorg Med Chem Lett. 2013 Feb 15;23(4):1046-50. doi: 10.1016/j.bmcl.2012.12.013., Epub 2012 Dec 20. PMID:23312472<ref>PMID:23312472</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Mus musculus]] | [[Category: Mus musculus]] | ||
[[Category: Receptor protein-tyrosine kinase]] | [[Category: Receptor protein-tyrosine kinase]] | ||
[[Category: Kohrt, J | [[Category: Kohrt, J]] | ||
[[Category: Ohren, J F | [[Category: Ohren, J F]] | ||
[[Category: Perrin, L A | [[Category: Perrin, L A]] | ||
[[Category: Powell, N A | [[Category: Powell, N A]] | ||
[[Category: Phosphotransferase]] | [[Category: Phosphotransferase]] | ||
[[Category: Receptor protein tyrosine kinase]] | [[Category: Receptor protein tyrosine kinase]] | ||
[[Category: Transferase-transferase inhibitor complex]] | [[Category: Transferase-transferase inhibitor complex]] | ||
