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Rapid discovery of drug target engagement by isothermal shift assay

ABSTRACT: Determining protein targets directly bound by drug molecules remains challenging. Here we present the isothermal shift assay, iTSA, for rapid unbiased identification of drug targets. Compared with thermal proteome profiling, the prevailing method for target engagement, iTSA offers a simplified workflow, 4- fold higher throughput, and a multiplexed experimental design with higher replication. We demonstrate its application to determination of target engagement for several kinase inhibitors in lysates and living cells.

INSTRUMENT(S): Orbitrap Fusion

ORGANISM(S): Homo Sapiens (ncbitaxon:9606)

SUBMITTER: William Old

PROVIDER: MSV000083640 | MassIVE | Thu Mar 28 10:27:00 GMT 2019

SECONDARY ACCESSION(S): PXD013293

REPOSITORIES: MassIVE

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