4mbj
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4mbj]] 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=4MBJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4MBJ FirstGlance]. <br> | <table><tr><td colspan='2'>[[4mbj]] 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=4MBJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4MBJ FirstGlance]. <br> | ||
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DFS:2,6-DIFLUORO-N-(1H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-3-[(PROPYLSULFONYL)AMINO]BENZAMIDE'>DFS</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]] 3.6Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DFS:2,6-DIFLUORO-N-(1H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-3-[(PROPYLSULFONYL)AMINO]BENZAMIDE'>DFS</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=4mbj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mbj OCA], [https://pdbe.org/4mbj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4mbj RCSB], [https://www.ebi.ac.uk/pdbsum/4mbj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4mbj 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=4mbj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mbj OCA], [https://pdbe.org/4mbj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4mbj RCSB], [https://www.ebi.ac.uk/pdbsum/4mbj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4mbj 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 == | ||
| - | This Letter details the synthesis and evaluation of imidazo[4,5-b]pyridines as inhibitors of B-Raf kinase. These compounds bind in a DFG-in, alphaC-helix out conformation of B-Raf, which is a binding mode associated with significant kinase selectivity. Structure-activity relationship studies involved optimization of the ATP-cleft binding region of these molecules, and led to compound 23, an inhibitor with excellent enzyme/cell potency, and kinase selectivity. | ||
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| - | Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase.,Newhouse BJ, Wenglowsky S, Grina J, Laird ER, Voegtli WC, Ren L, Ahrendt K, Buckmelter A, Gloor SL, Klopfenstein N, Rudolph J, Wen Z, Li X, Feng B Bioorg Med Chem Lett. 2013 Aug 29. pii: S0960-894X(13)01026-3. doi:, 10.1016/j.bmcl.2013.08.086. PMID:24042006<ref>PMID:24042006</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 4mbj" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
Current revision
Human B-Raf Kinase Domain in Complex with an Imidazopyridine-based Inhibitor
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