4w9w
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 4w9w is ON HOLD Authors: Sorrell, F.J., Elkins, J.M., Krojer, T., Savitsky, P., Williams, E., Von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountr...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal Structure of BMP-2-inducible kinase in complex with small molecule AZD-7762== | |
| + | <StructureSection load='4w9w' size='340' side='right'caption='[[4w9w]], [[Resolution|resolution]] 1.72Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4w9w]] is a 1 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=4W9W OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4W9W FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.72Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=YDJ:5-(3-FLUOROPHENYL)-N-[(3S)-3-PIPERIDYL]-3-UREIDO-THIOPHENE-2-CARBOXAMIDE'>YDJ</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=4w9w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4w9w OCA], [https://pdbe.org/4w9w PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4w9w RCSB], [https://www.ebi.ac.uk/pdbsum/4w9w PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4w9w ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/BMP2K_HUMAN BMP2K_HUMAN] May be involved in osteoblast differentiation. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The highly diverse Numb-associated kinase (NAK) family has been linked to broad cellular functions including receptor-mediated endocytosis, Notch pathway modulation, osteoblast differentiation, and dendrite morphogenesis. Consequently, NAK kinases play a key role in a diverse range of diseases from Parkinson's and prostate cancer to HIV. Due to the plasticity of this kinase family, NAK kinases are often inhibited by approved or investigational drugs and have been associated with side effects, but they are also potential drug targets. The presence of cysteine residues in some NAK family members provides the possibility for selective targeting via covalent inhibition. Here we report the first high-resolution structures of kinases AAK1 and BIKE in complex with two drug candidates. The presented data allow a comprehensive structural characterization of the NAK kinase family and provide the basis for rational design of selective NAK inhibitors. | ||
| - | + | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.,Sorrell FJ, Szklarz M, Abdul Azeez KR, Elkins JM, Knapp S Structure. 2016 Jan 29. pii: S0969-2126(16)00008-3. doi:, 10.1016/j.str.2015.12.015. PMID:26853940<ref>PMID:26853940</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| + | <div class="pdbe-citations 4w9w" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Arrowsmith CH]] | ||
| + | [[Category: Bountra C]] | ||
| + | [[Category: Edwards AM]] | ||
| + | [[Category: Elkins JM]] | ||
| + | [[Category: Knapp S]] | ||
| + | [[Category: Krojer T]] | ||
| + | [[Category: Savitsky P]] | ||
| + | [[Category: Sorrell FJ]] | ||
| + | [[Category: Williams E]] | ||
| + | [[Category: Von Delft F]] | ||
Current revision
Crystal Structure of BMP-2-inducible kinase in complex with small molecule AZD-7762
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Categories: Homo sapiens | Large Structures | Arrowsmith CH | Bountra C | Edwards AM | Elkins JM | Knapp S | Krojer T | Savitsky P | Sorrell FJ | Williams E | Von Delft F
