Abstract
Modulation of protein–protein interactions (PPIs) is becoming increasingly important in drug discovery and chemical biology. While a few years ago this ‘target class’ was deemed to be largely undruggable an impressing number of publications and success stories now show that targeting PPIs with small, drug-like molecules indeed is a feasible approach. Here, we summarize the current state of small-molecule inhibition and stabilization of PPIs and review the active molecules from a structural and medicinal chemistry angle, especially focusing on the key examples of iNOS, LFA-1 and 14–3–3.
Financial & competing interests disclosure
The authors are very grateful to the organizations that funded their research: The Deutsche Forschungsgemeinschaft (DFG, grants OT 414/2–1 and SFB 1093) and the European Commission (IAPP, Project 286418). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.