Abstract: Provided herein is a method and system for detecting kinase activity, comprising: providing one or more mutated kinases, wherein the one or more mutated kinases comprise a mutation that enlarges an ATP binding pocket of the kinase; contacting the one or more mutated kinases with an ATP or ADP analog-nanoparticle conjugate capable of intracellular delivery of the ATP or ADP analog-nanoparticle conjugate, wherein the ATP or ADP analog comprises a detectable label; assaying the one or more mutated kinases under conditions in which the ATP or ADP analog-nanoparticle conjugate contacts the one or more mutated kinases, wherein the one or more kinases react to transfer the detectable label to the substrate, wherein the ATP analog only fluoresces upon contact with the ATP binding pocket of the kinase.

Abstract: The present invention includes method and system for detecting kinase activity in vivo, comprising: providing a cell that comprises one or more mutated kinases, wherein the one or more mutated kinases comprise a mutation that enlarges an ATP binding pocket of the kinase; contacting the cell with an ATP analog-nanoparticle conjugate capable of intracellular delivery of the ATP analog-nanoparticle conjugate, wherein the ATP analog comprises a detectable label; culturing the cells under conditions in which the ATP analog-nanoparticle conjugate contacts the one or more mutated kinases in cellulo, wherein the detectable label is transferred from the ATP analog-nanoparticle conjugate to a substrate of the one or more mutated kinases, wherein the one or more kinases react to transfer the detectable label to the substrate.