Identification of a Small Compound Targeting PKM2-Regulated Signaling Using 2D Gel Electrophoresis-Based Proteome-wide CETSA (Cell Chemical Biology)

Nagasawa et al. developed a proteome-wide cellular thermal shift assay (CETSA) method `2DE-CETSA` to identify thermal stability-shifted proteins due to interactions with a small compound. Using 2DE-CETSA, they have shown that an anti-cancer compound NPD10084 induced thermal destabilization of PKM2. NPD10084 disrupted the PKM2 complex and inhibited downstream signaling.