p300 and CBP are paralogous epigenetic regulators and promising therapeutic targets for which TPD offers the potential to achieve paralog-selective degradation.
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.
Heat shock protein 90, a widely expressed molecular chaperone, has emerged as a promising anticancer target due to its crucial role in stabilizing and regulating the functions of numerous client proteins including tumor-associated proteins.
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.