Fragment screening using biolayer interferometry reveals ligands targeting the SHP-motif binding site of the AAA+ ATPase p97

Abstract

The AAA+ ATPase p97 protein is thought to be a potential anticancer target, but direct targeting on its ATPase function has not proven to be a successful strategy in clinical trials due to lack of selectivity. Here, the authors use biolayer interferometry-based fragment screening to identify ligands for the development of protein-protein interaction inhibitors by targeting the SHP-motif as a cofactor binding site in the N-domain of p97.