The cellular thermal shift assay: a novel biophysical assay for in situ drug target engagement and mechanistic biomarker studies
D Martinez Molina, P Nordlund - Annual review of …, 2016 - annualreviews.org
A drug must engage its intended target to achieve its therapeutic effect. However,
conclusively measuring target engagement (TE) in situ is challenging. This complicates
preclinical development and is considered a key factor in the high rate of attrition in clinical
trials. Here, we discuss a recently developed, label-free, biophysical assay, the cellular
thermal shift assay (CETSA), which facilitates the direct assessment of TE in cells and
tissues at various stages of drug development. CETSA also reveals biochemical events …
conclusively measuring target engagement (TE) in situ is challenging. This complicates
preclinical development and is considered a key factor in the high rate of attrition in clinical
trials. Here, we discuss a recently developed, label-free, biophysical assay, the cellular
thermal shift assay (CETSA), which facilitates the direct assessment of TE in cells and
tissues at various stages of drug development. CETSA also reveals biochemical events …
