4yht
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4yht]] 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=4YHT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YHT FirstGlance]. <br> | <table><tr><td colspan='2'>[[4yht]] 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=4YHT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YHT FirstGlance]. <br> | ||
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4EF:3-[(5-CHLORO-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)AMINO]-N-METHYL-4-(MORPHOLIN-4-YL)BENZENESULFONAMIDE'>4EF</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.05Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4EF:3-[(5-CHLORO-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)AMINO]-N-METHYL-4-(MORPHOLIN-4-YL)BENZENESULFONAMIDE'>4EF</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</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=4yht FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yht OCA], [https://pdbe.org/4yht PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yht RCSB], [https://www.ebi.ac.uk/pdbsum/4yht PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yht ProSAT]</span></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=4yht FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yht OCA], [https://pdbe.org/4yht PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yht RCSB], [https://www.ebi.ac.uk/pdbsum/4yht PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yht ProSAT]</span></td></tr> | ||
</table> | </table> | ||
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== Function == | == Function == | ||
[https://www.uniprot.org/uniprot/BRAF_HUMAN BRAF_HUMAN] Involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. | [https://www.uniprot.org/uniprot/BRAF_HUMAN BRAF_HUMAN] Involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | A series of selective TNNI3K inhibitors were developed by modifying the hinge-binding heterocycle of a previously reported dual TNNI3K/B-Raf inhibitor. The resulting quinazoline-containing compounds exhibit a large preference (up to 250-fold) for binding to TNNI3K versus B-Raf, are useful probes for elucidating the biological pathways associated with TNNI3K, and are leads for discovering novel cardiac medicines. GSK114 emerged as a leading inhibitor, displaying significant bias (40-fold) for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity, and adequate oral exposure to enable its use in cellular and in vivo studies. | ||
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| - | GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.,Lawhorn BG, Philp J, Graves AP, Shewchuk L, Holt DA, Gatto GJ Jr, Kallander LS Bioorg Med Chem Lett. 2016 Jul 15;26(14):3355-8. doi: 10.1016/j.bmcl.2016.05.033., Epub 2016 May 14. PMID:27246618<ref>PMID:27246618</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 4yht" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
Current revision
bRaf complexed with an inhibitor
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