Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges.
Proteolysis targeting chimeras (PROTACs) are heterobifunctional compounds with molecular weights and other properties that lie outside the classic 'rule-of-five' space. Consequently, PROTACs have unique challenges associated with their development as potential therapeutic agents. This review summarizes and analyzes a representative set of recent PROTACs and highlights some of the potential future challenges facing this promising modality.
['Edmondson|Scott D|SD|', 'Yang|Bin|B|', 'Fallan|Charlene|C|']
D002678:Chimera D055808:Drug Discovery D006801:Humans D059748:Proteolysis
Proteolysis targeting chimeras PROTACs Beyond rule-of-five Absorption Degradation Oral bioavailability bRo5