Restoration of FLT-3 speciific cytotoxcity despite AGP binding (IMAGE)
Caption
2,800 compounds from the Johns Hopkins Drug Library were screened for the ability to restore the activity of midostaurin in the presence of inhibiting amounts of human AGP. Most compounds had no effect upon FLT3 (blue dots falling along the diagonal line); however, a subset of the compounds (orange dots) appear to restore the ability of midostaurin to inhibit FLT3 and kill the cells. The authors also screened the compounds for their ability to bind to AGP (squares). Compounds that both restore activity and bind to AGP (squared orange dots) may serve as AGP decoys to rescue midostaurin and other similar drugs from AGP inhibition.
Credit
David Young, M.D., Ph.D., and Donald Small, M.D., Ph.D.
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Original content