Focal adhesion kinase

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Function

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[1].

Relevance

FAK is overexpressed in many tumor cells. Hence they are investigated as anti-tumor drug targets[2].

Structural insights

FAK ATP-binding site is the [3].

3D Structures of focal adhesion kinase

Focal adhesion kinase 3D structures


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

Drag the structure with the mouse to rotate

ReferencesReferences

  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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