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Publication and contact information

Assays & screens

Measuring target engagement in samples

An assay to detect ligand binding in cells could be used to assess target engagement during preclinical and clinical drug development. In cell lysates and in mouse cells and tissues, the cellular thermal shift assay (CETSA) was used to monitor small molecule-induced stabilization of their protein targets by measuring shifts in protein thermal melting curves. In samples from mice, a methionine aminopeptidase 2 (MetAP2) inhibitor shifted the thermal melting curve. Next steps include developing CETSA to monitor target engagement during clinical trials to help explain responders and nonresponders and as a diagnostic tool to inform patient-specific drug selection and dosing (see Engaging drug discovery, page 1).

SciBX 6(30); doi:10.1038/scibx.2013.804
Published online Aug. 8, 2013

Patented; available for licensing from Pelago Bioscience AB

Molina, D.M. et al. Science; published online July 5, 2013;
Contact: Pär Nordlund, Karolinska Institute, Stockholm, Sweden