Proteolysis targeting chimeras (PROTACs) for epigenetics research.

Current Opinion in Chemical Biology
Anja VogelmannManfred Jung

Abstract

Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules and allow selective protein degradation by addressing the natural ubiquitin proteasome system. As this new strategy of chemically induced protein degradation can serve as a biological tool and provides new possibilities for drug discovery, it has been applied to a variety of targets including (nuclear) receptors, kinases, and epigenetic proteins. A lot of PROTACs have already been designed in the field of epigenetics, and their synthesis and characterization highly contributed to structural optimization and improved mechanistic understanding of these molecules. In this review, we will discuss and summarize recent advances in PROTAC discovery with focus on epigenetic targets.

Citations

Aug 5, 2020·Epigenetics : Official Journal of the DNA Methylation Society·Ana Rita CardosoCarmen Jerónimo
Nov 16, 2020·The FEBS Journal·Dilşad H ArabacıTamer T Önder
Oct 22, 2020·Expert Opinion on Therapeutic Patents·Andrew B BenowitzJohn D Harling
Oct 15, 2020·Cellular and Molecular Life Sciences : CMLS·Dejun LiuWenzhang Zha
Feb 21, 2021·The Journal of Allergy and Clinical Immunology·Nadezhda Camacho-OrdonezBodo Grimbacher
Jul 2, 2020·Journal of Medicinal Chemistry·Terence C S HoA Ganesan
Sep 1, 2020·Biochemical Pharmacology·Yuqing LiangKui Cheng
Apr 4, 2021·Journal of Clinical Medicine·Frédéric SoysouvanhRobert Ballotti
May 19, 2021·Nature Reviews. Cancer·Shuai ZhaoGang Greg Wang
Jun 22, 2021·Annual Review of Biochemistry·John D Bagert, Tom W Muir
Aug 17, 2020·Cell Chemical Biology·Dhanusha A Nalawansha, Craig M Crews
Aug 26, 2021·Biological Chemistry·Anna-Theresa BlaslMichael Lammers
Sep 16, 2021·Journal of Medicinal Chemistry·Lucienne Juillerat-JeanneretDela Golshayan

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