A perspective on the discovery of enzyme activators

Enzyme activation remains a largely under-represented and poorly exploited area of drug discovery despite some key literature examples of the successful application of enzyme activators by various mechanisms and their importance in a wide range of therapeutic interventions. Here we describe the background nomenclature, present the current position of this field of drug discovery and discuss the challenges of hit identification for enzyme activation, as well as our perspectives on the approaches needed to overcome these challenges in early drug discovery.

Automated summary

The article discusses the under-representation and under-utilization of enzyme activation in drug discovery, despite its importance and proven success in therapeutic interventions. It also highlights the challenges in identifying hits for enzyme activation and the approaches needed to overcome these challenges in early drug discovery.