Rebecca Stevens, James D. F. Thompson, Julie C. L. Fournier, Glenn A. Burley, David J. Battersby and Afjal H. Miah
Chem. Soc. Rev., 2024,53, 4838-4861
Abstract
In this review we highlight how the synthesis of degraders has evolved in recent years, in particular the application of high-throughput chemistry and screening approaches such as D2B and DEL technologies to expedite discovery timelines.
Ce Yang, Ravi Tripathi and Binghe Wang
RSC Chem. Biol., 2024,5, 189-197
Abstract
This review discusses leveraging click chemistry to address unmet needs in PROTAC development.
Md Kabir, Xufen Yu, H. Ümit Kaniskan and Jian Jin
Chem. Soc. Rev., 2023,52, 4313-4342
From themed collection:
Modalities of induced proximity pharmacology: Degraders and Beyond themed collection
Abstract
This review summarizes the past and present advances in developing degraders of epigenetic targets which play critical roles in many crucial biological pathways and therefore, targeted for the discovery of therapeutics.
Yossra Gharbi and Rocío Mercado
Digital Discovery, 2024,3, 2158-2176
Abstract
Machine learning (ML) accelerates PROTAC design by optimizing linkers and protein–ligase interactions, enabling selective protein degradation for therapeutic applications, particularly targeting previously undruggable proteins.
Urvashi Patel, Joshua P. Smalley and James T. Hodgkinson
RSC Chem. Biol., 2023,4, 623-634
From themed collection:
Medicinal Chemistry Small Molecule Probes
Abstract
A review on current proteolysis targeting chimeras (PROTACs) as chemical probes for histone deacetylase (HDAC) enzymes.