Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five'chemical space: Recent progress and future challenges
SD Edmondson, B Yang, C Fallan - Bioorganic & Medicinal Chemistry …, 2019 - Elsevier
SD Edmondson, B Yang, C Fallan
Bioorganic & Medicinal Chemistry Letters, 2019•ElsevierProteolysis 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.
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.
Abstract
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.
Elsevier