Research Progress on Oral Proteolysis Targeting Chimera Drugs

Proteolysis targeting chimera（PROTAC） technology is an emerging drug discovery strategy capable of targeting "undruggable" targets that are difficult to be intervened by traditional small molecule drugs. It has become a groundbreaking technology and a research hotspot in the field of induced protein degradation. Although PROTACs have shown significant potential for clinical applications,their special molecular structures still pose substantial challenges on oral bioavailability. This review summarizes the research progress on oral PROTACs and discusses strategies to improve their oral bioavailability from the medicinal chemistry perspective.