6gcw
From Proteopedia
(Difference between revisions)
| Line 1: | Line 1: | ||
| - | '''Unreleased structure''' | ||
| - | + | ==Focal Adhesion Kinase catalytic domain in complex with irreversible inhibitor== | |
| - | + | <StructureSection load='6gcw' size='340' side='right'caption='[[6gcw]], [[Resolution|resolution]] 2.00Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[6gcw]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6GCW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6GCW FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EUQ:2-[[5-chloranyl-2-[[4-[[[1-[2-(propanoylamino)ethyl]-1,2,3-triazol-4-yl]methylamino]methyl]phenyl]amino]pyrimidin-4-yl]amino]-~{N}-methyl-benzamide'>EUQ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | |
| - | [[Category: | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6gcr|6gcr]], [[6gcx|6gcx]]</td></tr> |
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6gcw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6gcw OCA], [http://pdbe.org/6gcw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6gcw RCSB], [http://www.ebi.ac.uk/pdbsum/6gcw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6gcw ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/FAK1_CHICK FAK1_CHICK]] Non-receptor protein-tyrosine kinase that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adhesions and cell protrusions, cell cycle progression, cell proliferation and apoptosis. Required for early embryonic development, embryonic angiogenesis, normal cardiomyocyte migration and proliferation, and normal heart development. Regulates axon growth and neuronal cell migration, axon branching and synapse formation; required for normal development of the nervous system. Plays a role in osteogenesis and differentiation of osteoblasts. Functions in integrin signal transduction, but also in signaling downstream of numerous growth factor receptors, G-protein coupled receptors (GPCR), ephrin receptors, netrin receptors and LDL receptors. Forms multisubunit signaling complexes with SRC and SRC family members upon activation; this leads to the phosphorylation of additional tyrosine residues, creating binding sites for scaffold proteins, effectors and substrates. Regulates numerous signaling pathways. Promotes activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascade. Promotes activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling cascade. Promotes localized and transient activation of guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs), and thereby modulates the activity of Rho family GTPases. Signaling via CAS family members mediates activation of RAC1. Regulates P53/TP53 activity and stability. Phosphorylates SRC; this increases SRC kinase activity. Isoform 2 (FRNK) does not contain a kinase domain and inhibits PTK2/FAK1 phosphorylation and signaling.<ref>PMID:15494733</ref> <ref>PMID:15494734</ref> <ref>PMID:15494732</ref> <ref>PMID:20705914</ref> <ref>PMID:21852560</ref> <ref>PMID:21937583</ref> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Non-specific protein-tyrosine kinase]] | ||
| + | [[Category: Acebron-Garcia-de-Eulate, M]] | ||
| + | [[Category: Chen, H]] | ||
| + | [[Category: Coumoul, X]] | ||
| + | [[Category: Dawson, J]] | ||
| + | [[Category: Etheve-Quelquejeu, M]] | ||
| + | [[Category: Frame, M C]] | ||
| + | [[Category: Garbay, C]] | ||
| + | [[Category: Li, B]] | ||
| + | [[Category: Lietha, D]] | ||
| + | [[Category: Tomkiewicz-Raulet, C]] | ||
| + | [[Category: Yen-Pon, E]] | ||
| + | [[Category: 4-pyrimidine derivative]] | ||
| + | [[Category: Cell adhesion]] | ||
| + | [[Category: Focal adhesion kinase cell adhesion signalling irreversible inhibitor 2]] | ||
Revision as of 08:47, 1 May 2019
Focal Adhesion Kinase catalytic domain in complex with irreversible inhibitor
| |||||||||||
Categories: Large Structures | Non-specific protein-tyrosine kinase | Acebron-Garcia-de-Eulate, M | Chen, H | Coumoul, X | Dawson, J | Etheve-Quelquejeu, M | Frame, M C | Garbay, C | Li, B | Lietha, D | Tomkiewicz-Raulet, C | Yen-Pon, E | 4-pyrimidine derivative | Cell adhesion | Focal adhesion kinase cell adhesion signalling irreversible inhibitor 2
