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The application of PROTAC in HDAC.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2023 Nov 15; Vol. 260, pp. 115746. Date of Electronic Publication: 2023 Aug 19. - Publication Year :
- 2023
-
Abstract
- Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great opportunities for scientific research and industrial applications. Histone deacetylase (HDAC)-PROTAC has been widely developed since the first report of its ability to induce the degradation of SIRT2 in 2017. To date, ten of the eighteen HDACs (HDACs 1-8, HDAC10, and SIRT2) have been successfully targeted and degraded by HDAC-PROTACs. HDAC-PROTACs surpass traditional HDAC inhibitors in many aspects, such as higher selectivity, more potent antiproliferative activity, and the ability to disrupt the enzyme-independent functions of a multifunctional protein and overcome drug resistance. Rationally designing HDAC-PROTACs is a main challenge in development because slight variations in chemical structure can lead to drastic effects on the efficiency and selectivity of the degradation. In the future, HDAC-PROTACs can potentially be involved in clinical research with the support of the increased amount of in vivo data, pharmacokinetic evaluation, and pharmacological studies.<br />Competing Interests: Declaration of competing interest All authors declare no competing financial interest.<br /> (Copyright © 2023 Elsevier Masson SAS. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 260
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 37607440
- Full Text :
- https://doi.org/10.1016/j.ejmech.2023.115746