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5ct7
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[5ct7]] 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=5CT7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5CT7 FirstGlance]. <br> | <table><tr><td colspan='2'>[[5ct7]] 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=5CT7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5CT7 FirstGlance]. <br> | ||
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=55J:1-METHYL-5-({2-[5-(TRIFLUOROMETHYL)-1H-IMIDAZOL-2-YL]PYRIDIN-4-YL}OXY)-N-[4-(TRIFLUOROMETHYL)PHENYL]-1H-BENZIMIDAZOL-2-AMINE'>55J</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]] 3.17Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=55J:1-METHYL-5-({2-[5-(TRIFLUOROMETHYL)-1H-IMIDAZOL-2-YL]PYRIDIN-4-YL}OXY)-N-[4-(TRIFLUOROMETHYL)PHENYL]-1H-BENZIMIDAZOL-2-AMINE'>55J</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=5ct7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ct7 OCA], [https://pdbe.org/5ct7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ct7 RCSB], [https://www.ebi.ac.uk/pdbsum/5ct7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ct7 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=5ct7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ct7 OCA], [https://pdbe.org/5ct7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ct7 RCSB], [https://www.ebi.ac.uk/pdbsum/5ct7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ct7 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 == | ||
| - | Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent cancers. We report the development of imidazo-benzimidazoles as potent B-RAF inhibitors. Robust in vivo efficacy coupled with correlating pharmacokinetic/pharmacodynamic (PKPD) and PD-efficacy relationships led to the identification of RAF265, 1, which has advanced into clinical trials. | ||
| - | |||
| - | Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.,Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D ACS Med Chem Lett. 2015 Aug 3;6(9):961-5. doi: 10.1021/ml500526p. eCollection, 2015 Sep 10. PMID:26396681<ref>PMID:26396681</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 5ct7" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
Current revision
BRAF in Complex with RAF265
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