2. Academic Validation
  3. PROTACs in Epigenetic Cancer Therapy: Current Status and Future Opportunities

PROTACs in Epigenetic Cancer Therapy: Current Status and Future Opportunities

  • Molecules. 2023 Jan 26;28(3):1217. doi: 10.3390/molecules28031217.
Xuelian Liu 1 2 3,  Anjin Wang 1 2 3,  Yuying Shi 1 2 3,  Mengyuan Dai 1 2 3,  Miao Liu 4,  Hong-Bing Cai 1 2 3
Affiliations

Affiliations

  • 1 Department of Gynecological Oncology, Zhongnan Hospital of Wuhan University, Wuhan 430071, China.
  • 2 Hubei Key Laboratory of Tumor Biological Behaviors, Wuhan 430071, China.
  • 3 Hubei Cancer Clinical Study Center, Wuhan 430071, China.
  • 4 Department of Pathology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.
PMID: 36770884 DOI: 10.3390/molecules28031217
Abstract

The epigenetic regulation of gene functions has been proven to be strongly associated with the development and progression of Cancer. Reprogramming the Cancer epigenome landscape is one of the most promising target therapies in both treatments and in reversing drug resistance. Proteolytic targeted chimeras (PROTACs) are an emerging therapeutic modality for selective degradation via the native ubiquitin-proteasome system. Rapid advances in PROTACs have facilitated the exploration of targeting epigenetic proteins, a lot of PROTAC degraders have already been designed in the field of epigenetic Cancer therapy, and PROTACs targeting epigenetic proteins can better exploit target druggability and improve the mechanistic understanding of the epigenetic regulation of Cancer. Thus, this review focuses on the progress made in the development of PROTAC degraders and PROTAC drugs targeting Epigenetics in Cancer and discusses challenges and future opportunities for the field.

Keywords

PROTACs; cancer therapy; epigenetics; protein degradation.

Figures
Products