Innovative, combinatorial and high-throughput approaches to degrader synthesis
Rebecca Stevens, James D. F. Thompson, Julie C. L. Fournier, Glenn A. Burley, David Battersby, Afjal H. Miah
Abstract
induced proximity. Their optimisation thus far has often been largely empirical, requiring the synthesis and screening of a large number of analogues. In addition, the synthesis and development of degraders is often challenging, leading to lengthy optimisation campaigns to deliver candidate-quality compounds. This review highlights how the synthesis of degraders has evolved in recent years, in particular focusing on means of applying high-throughput chemistry and screening approaches to expedite these timelines, which we anticipate to be valuable in shaping the future of degrader optimisation campaigns.
Topics & Concepts
ThroughputCombinatorial synthesisComputer scienceCombinatorial chemistryChemistryTelecommunicationsWirelessProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysHistone Deacetylase Inhibitors Research