Focal adhesion kinase

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<StructureSection load='2jkk' size='350' side='right' scene='' caption='Focal adhesion kinase 1 kinase domain complex with pyrimidine derivative inhibitor and sulfate (PDB code [[2jkk]]) '>
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<StructureSection load='2jkk' size='350' side='right' scene='48/480805/Cv/1' caption='Focal adhesion kinase 1 kinase domain complex with pyrimidine derivative inhibitor and sulfate (PDB code [[2jkk]]) '>
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== Function ==
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For details on '''focal adhesion kinase or protein tyrosine kinase 2β (PTK2)''' see [[Molecular Playground/FAK]]<ref>PMID:8747466</ref>.
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'''Focal adhesion kinase''' (FAK) is involved in cellular adhesion. During apoptosis, FAK is cleaved into 2 fragments. The smaller fragment is associated with death signaling. For details on '''focal adhesion kinase or protein tyrosine kinase 2β (PTK2)''' see [[Molecular Playground/FAK]]<ref>PMID:15688067</ref>.
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</StructureSection>
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== 3D Structures of focal adhesion kinase ==
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Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
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== Relevance ==
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{{#tree:id=OrganizedByTopic|openlevels=0|
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*Focal adhesion kinase 1 (FAK1)
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FAK is overexpressed in many tumor cells. Hence they are investigated as anti-tumor drug targets<ref>PMID:22075057</ref>.
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*''FAK1 targeting domain''
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== Structural insights ==
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**[[1k04]], [[1k05]], [[3s9o]], [[2l6h]], [[2l6g]], [[2l6f]] – hFAK1 – human<br />
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FAK ATP-binding site is the <scene name='48/480805/Cv/5'>location of inhibitor binding</scene><ref>PMID:19030106</ref>.
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**[[1k40]] – FAK1 – mouse<br />
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**[[1ow6]], [[1ow7]] - hFAK1 + paxillin LD4 motif<br />
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**[[1ow8]] - hFAK1 + paxillin LD2 motif<br />
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**[[3b71]] - hFAK1 + ADP + ATP<BR />
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**[[1ktm]], [[1qvx]], [[1pv3]] - cFAK1 – chicken – NMR
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*''FAK1 kinase domain''
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== 3D Structures of focal adhesion kinase ==
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[[Focal adhesion kinase 3D structures]]
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**[[1mp8]] - hFAK1 <br />
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</StructureSection>
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**[[2etm]], [[3bz3]], [[4gu9]], [[4kab]], [[4k9y]], [[4i4e]], [[4i4f]], [[4k8a]], [[4gu6]], [[4brx]], [[4ebv]], [[4ebw]], [[3pxk]], [[4q9s]] - hFAK1 + inhibitor<br />
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**[[4kao]] - hFAK1 (mutant) + pyrazole derivative<br />
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**[[2ijm]] - hFAK1 + ADP + ATP<BR />
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**[[4d4r]], [[4d4s]], [[4d4v]], [[4d4y]], [[4d55]], [[4d5h]], [[4d5k]] - cFAK1<br />
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**[[2j0l]] - cFAK1 phosphorylated<br />
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**[[2jkk]], [[2jkm]], [[2jko]], [[2jkq]], [[4d58]] - cFAK1 + pyrimidine derivative<br />
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**[[4c7t]] - cFAK1 + inhibitor<br />
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*''FAK1 FERM domain''
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**[[2j0j]], [[2j0k]], [[2j0m]] - cFAK1 kinase + FERM domains<br />
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**[[2aeh]], [[2al6]] - cFAK1<br />
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**[[3zdt]] - cFAK1 (mutant)<br />
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**[[4cye]] - hFAK1<br />
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**[[4ny0]] - hFAK1 (mutant)<br />
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*Focal adhesion kinase 2 (FAK2) See Pyk2 in [[Tyrosine kinase]]
 
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}}
 
== References ==
== References ==
<references/>
<references/>
[[Category:Topic Page]]
[[Category:Topic Page]]

Current revision

Focal adhesion kinase 1 kinase domain complex with pyrimidine derivative inhibitor and sulfate (PDB code 2jkk)

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References

  1. ↑ Mitra SK, Hanson DA, Schlaepfer DD. Focal adhesion kinase: in command and control of cell motility. Nat Rev Mol Cell Biol. 2005 Jan;6(1):56-68. PMID:15688067 doi:http://dx.doi.org/10.1038/nrm1549
  2. ↑ Cabrita MA, Jones LM, Quizi JL, Sabourin LA, McKay BC, Addison CL. Focal adhesion kinase inhibitors are potent anti-angiogenic agents. Mol Oncol. 2011 Dec;5(6):517-26. doi: 10.1016/j.molonc.2011.10.004. Epub 2011 Oct, 20. PMID:22075057 doi:http://dx.doi.org/10.1016/j.molonc.2011.10.004
  3. ↑ Lietha D, Eck MJ. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS ONE. 2008;3(11):e3800. Epub 2008 Nov 24. PMID:19030106 doi:10.1371/journal.pone.0003800

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Michal Harel, Alexander Berchansky

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