A systematic investigation of cyclic imide stereoisomers in small molecules, peptides, and proteins, examining their racemization, CRBN engagement, ternary complex formation in vitro, and resulting degradation outcomes in cells.
This review summarizes recent synthetic advances for glutarimide scaffolds enabling cereblon-mediated targeted protein degradation.
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.
EZH2, a histone methyltransferase and the catalytic subunit of the polycomb repressive complex 2 (PRC2), plays a pivotal role in tumor epigenetics through transcriptional repression of tumor suppressor genes.
The first PROTAC degrader of ASK1, dASK1-VHL (60), was rationally designed and validated via in vitro assays and PK studies, demonstrating therapeutic efficacy in an MCD diet-induced MASH mouse model, underscoring its promise in metabolic diseases.