Positioning High-Throughput CETSA in Early Drug Discovery through Screening against B-Raf and PARP1.

ABSTRACT: Methods to measure cellular target engagement are increasingly being used in early drug discovery. The Cellular Thermal Shift Assay (CETSA) is one such method. CETSA can investigate target engagement by measuring changes in protein thermal stability upon compound binding within the intracellular environment. It can be performed in high-throughput, microplate-based formats to enable broader application to early drug discovery campaigns, though high-throughput forms of CETSA have only been reported for a limited number of targets. CETSA offers the advantage of investigating the target of interest in its physiological environment and native state, but it is not clear yet how well this technology correlates to more established and conventional cellular and biochemical approaches widely used in

SUBMITTER: Shaw J 

PROVIDER: S-EPMC6484527 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature