Focal adhesion kinase

From Proteopedia

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spinqualitylabelsall models Focal adhesion kinase 1 kinase domain complex with pyrimidine derivative inhibitor and sulfate (PDB code 2jkk) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image 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

Updated on 18-May-2017

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