A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase.

ABSTRACT: Assessment of the interactions between a drug and its protein target in a physiologically relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery space. The Cellular Thermal Shift Assay (CETSA) enables such an assessment by quantifying the changes in the thermal stability of proteins upon ligand binding in intact cells. Here, we present the development and validation of a homogeneous, standardized, target-independent, and high-throughput (384- and 1536-well formats) CETSA platform that uses a split Nano Luciferase approach (SplitLuc CETSA). The broad applicability of the assay was demonstrated for diverse targets, and its performance was compared with independent biochemical and cell-based readouts using a set of well-characterized inhibitors. Moreove

SUBMITTER: Martinez NJ 

PROVIDER: S-EPMC6013488 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature