Mitoxantrone Targets the ATP-binding Site of FAK, Binds the FAK Kinase Domain and Decreases FAK, Pyk-2, c-Src, and IGF-1R In Vitro Kinase Activities

Golubovskaya V, et al., 13(4), 546-554, Anticancer Agents Med Chem, 2013

Computer modeling and cell viability assays were used to screen NCI small molecule compound database for compounds specific for the ATP binding site of FAK(Focal Adhesion Kinase), which is involved in multiple cellular functions and is a proposed therapeutic cancer target. A mitoxantrone derivative, compound A18, was identified and shown to inhibit cancer cell viability in vitro. The authors show compound A18 decreases FAK kinase function and kinase activity of other enzymes. The authors demonstrated using the Octet RED384 system and Super-Streptavidin biosensors that compound A18 binds to the FAK kinase domain.

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