PROTAC-mediated Target Degradation: A Paradigm Changer in Drug Discovery?

The recent successes of small-molecule-induced target degradation have generated considerable excitement in the pharmaceutical industry, which will be watching carefully as the first two assets progress through clinical trials. Proteolysis-targeting chimeras (PROTACs), a technology surfacing not more than a couple of decades ago, is in the process of revolutionizing drug discovery. This chapter will provide an introductory overview of the technology, highlighting some key milestones and speculating about future opportunities as well as challenges ahead.