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Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future
Scott D Edmondson1, Bin Yang1, Charlene Fallan2
1Medicinal Chemistry, Oncology, IMED Biotech Unit, AstraZeneca, Boston, MA, USA.
Bioorganic & Medicinal Chemistry Letters
|May 4, 2019
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.