3vap

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[[Image:3vap.png|left|200px]]
 
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==Synthesis and SAR Studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off target kinase selectivity==
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The line below this paragraph, containing "STRUCTURE_3vap", creates the "Structure Box" on the page.
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<StructureSection load='3vap' size='340' side='right'caption='[[3vap]], [[Resolution|resolution]] 2.66&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3vap]] 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=3VAP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3VAP FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.66&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0FY:3-(1-{2-[(3-FLUOROPYRIDINIUM-4-YL)AMINO]-2-OXOETHYL}-1H-PYRAZOL-4-YL)-6-METHYL-8-[(3-{[(1R,3R)-3-METHYLPIPERIDINIUM-1-YL]METHYL}-1,2-THIAZOL-5-YL)AMINO]IMIDAZO[1,2-A]PYRAZIN-1-IUM'>0FY</scene></td></tr>
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{{STRUCTURE_3vap| PDB=3vap | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3vap FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vap OCA], [https://pdbe.org/3vap PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3vap RCSB], [https://www.ebi.ac.uk/pdbsum/3vap PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3vap ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/AURKA_HUMAN AURKA_HUMAN] Mitotic serine/threonine kinases that contributes to the regulation of cell cycle progression. Associates with the centrosome and the spindle microtubules during mitosis and plays a critical role in various mitotic events including the establishment of mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. Required for initial activation of CDK1 at centrosomes. Phosphorylates numerous target proteins, including ARHGEF2, BORA, BRCA1, CDC25B, DLGP5, HDAC6, KIF2A, LATS2, NDEL1, PARD3, PPP1R2, PLK1, RASSF1, TACC3, p53/TP53 and TPX2. Regulates KIF2A tubulin depolymerase activity. Required for normal axon formation. Plays a role in microtubule remodeling during neurite extension. Important for microtubule formation and/or stabilization. Also acts as a key regulatory component of the p53/TP53 pathway, and particularly the checkpoint-response pathways critical for oncogenic transformation of cells, by phosphorylating and stabilizing p53/TP53. Phosphorylates its own inhibitors, the protein phosphatase type 1 (PP1) isoforms, to inhibit their activity. Necessary for proper cilia disassembly prior to mitosis.<ref>PMID:9606188</ref> <ref>PMID:11039908</ref> <ref>PMID:11551964</ref> <ref>PMID:12390251</ref> <ref>PMID:13678582</ref> <ref>PMID:14523000</ref> <ref>PMID:15147269</ref> <ref>PMID:14990569</ref> <ref>PMID:15128871</ref> <ref>PMID:14702041</ref> <ref>PMID:15987997</ref> <ref>PMID:18056443</ref> <ref>PMID:17604723</ref> <ref>PMID:17360485</ref> <ref>PMID:18615013</ref> <ref>PMID:19812038</ref> <ref>PMID:19351716</ref> <ref>PMID:19668197</ref> <ref>PMID:19357306</ref> <ref>PMID:20643351</ref> <ref>PMID:17125279</ref>
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===Synthesis and SAR Studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off target kinase selectivity===
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==See Also==
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*[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]]
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== References ==
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<references/>
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__TOC__
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(as it appears on PubMed at http://www.pubmed.gov), where 22503250 is the PubMed ID number.
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</StructureSection>
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{{ABSTRACT_PUBMED_22503250}}
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==About this Structure==
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[[3vap]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VAP OCA].
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==Reference==
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<ref group="xtra">PMID:022503250</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Large Structures]]
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[[Category: Basso, A D.]]
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[[Category: Basso AD]]
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[[Category: Belanger, D B.]]
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[[Category: Belanger DB]]
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[[Category: Fleming, M.]]
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[[Category: Fleming M]]
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[[Category: Gray, K.]]
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[[Category: Gray K]]
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[[Category: Hruza, A.]]
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[[Category: Hruza A]]
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[[Category: Peterson, L H.]]
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[[Category: Peterson LH]]
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[[Category: Rainka, M P.]]
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[[Category: Rainka MP]]
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[[Category: Siddiqui, M A.]]
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[[Category: Siddiqui MA]]
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[[Category: Voigt, J.]]
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[[Category: Voigt J]]
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[[Category: Voss, M E.]]
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[[Category: Voss ME]]
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[[Category: Cell cycle]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]
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[[Category: Transferase]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

Synthesis and SAR Studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off target kinase selectivity

PDB ID 3vap

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