Thursday, August 8, 2013
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Assays & screens
Measuring target engagement
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,
Published online Aug. 8, 2013
Patented; available for
licensing from Pelago
Molina, D.M. et al.
Science; published online July 5, 2013;
Contact: Pär Nordlund, Karolinska Institute, Stockholm, Sweden
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