4g9c
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4g9c]] 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=4G9C OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4G9C FirstGlance]. <br> | <table><tr><td colspan='2'>[[4g9c]] 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=4G9C OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4G9C FirstGlance]. <br> | ||
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0WP:3-{[3-(2-CYANOPROPAN-2-YL)BENZOYL]AMINO}-2,6-DIFLUORO-N-(3-METHOXY-2H-PYRAZOLO[3,4-B]PYRIDIN-5-YL)BENZAMIDE'>0WP</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]] 3.5Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0WP:3-{[3-(2-CYANOPROPAN-2-YL)BENZOYL]AMINO}-2,6-DIFLUORO-N-(3-METHOXY-2H-PYRAZOLO[3,4-B]PYRIDIN-5-YL)BENZAMIDE'>0WP</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=4g9c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g9c OCA], [https://pdbe.org/4g9c PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4g9c RCSB], [https://www.ebi.ac.uk/pdbsum/4g9c PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4g9c 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=4g9c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g9c OCA], [https://pdbe.org/4g9c PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4g9c RCSB], [https://www.ebi.ac.uk/pdbsum/4g9c PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4g9c 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 == | ||
| - | Cell potent inhibitors of B-Raf(V600E) that bind to the kinase in the DFG-out conformation are reported. These compounds utilize the hinge-binding group and lipophilic linker from a previously disclosed series of B-Raf(V600E) inhibitors that bind to the kinase in an atypical DFG-in, alphaC-helix-out conformation. This new series demonstrates that DFG-out kinase inhibitors can be rationally designed from related inhibitors which utilize an unconventional binding mode. Kinase selectivity profiles are compared. The pattern of kinase selectivity was found to be determined by the feature of the inhibitor which extends into the back pocket of the kinase and leads to the kinase conformation, rather than by the hinge-binding group or other minor modifications. | ||
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| - | Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.,Wenglowsky S, Moreno D, Laird ER, Gloor SL, Ren L, Risom T, Rudolph J, Sturgis HL, Voegtli WC Bioorg Med Chem Lett. 2012 Oct 1;22(19):6237-41. doi: 10.1016/j.bmcl.2012.08.007., Epub 2012 Aug 10. PMID:22954737<ref>PMID:22954737</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 4g9c" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
Current revision
Human B-Raf Kinase Domain bound to a Type II Pyrazolopyridine Inhibitor
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