» Articles » PMID: 26796965

Understanding the Complexity of Epigenetic Target Space

Overview
Journal J Med Chem
Specialty Chemistry
Date 2016 Jan 23
PMID 26796965
Citations 12
Authors
Affiliations
Soon will be listed here.
Abstract

The purpose of this review is to provide an overview of the complexity of the epigenetic target space. Chemical modifications of histones and nucleic acids constitute a key epigenetic mechanism. Whereas modifications such as methylation and acetylation are well-known, there are many additional, less explored modifications described here. The writers, readers and erasers of such diverse modifications, which constitute a major portion of the potential epigenetic target space, are discussed, in addition to the various other protein families that do not fall under these three categories. Finally, disease relevance and druggability of epigenetic targets are discussed with concluding remarks about the richness and diversity they will provide for future targeted therapies.

Citing Articles

Optimization of Resveratrol Used as a Scaffold to Design Histone Deacetylase (HDAC-1 and HDAC-2) Inhibitors.

Urias B, Pavan A, Albuquerque G, Prokopczyk I, Alves T, de Melo T Pharmaceuticals (Basel). 2022; 15(10).

PMID: 36297372 PMC: 9611521. DOI: 10.3390/ph15101260.


Palmitate-Triggered COX2/PGE2-Related Hyperinflammation in Dual-Stressed PdL Fibroblasts Is Mediated by Repressive H3K27 Trimethylation.

Schuldt L, Reimann M, von Brandenstein K, Steinmetz J, Doding A, Schulze-Spate U Cells. 2022; 11(6).

PMID: 35326406 PMC: 8946768. DOI: 10.3390/cells11060955.


Design, Synthesis, and Biological Evaluation of HDAC Degraders with CRBN E3 Ligase Ligands.

Lu Y, Sun D, Xiao D, Shao Y, Su M, Zhou Y Molecules. 2021; 26(23).

PMID: 34885822 PMC: 8658794. DOI: 10.3390/molecules26237241.


Regulation of the Methylation and Expression Levels of the BMPR2 Gene by SIN3a as a Novel Therapeutic Mechanism in Pulmonary Arterial Hypertension.

Bisserier M, Mathiyalagan P, Zhang S, Elmastour F, Dorfmuller P, Humbert M Circulation. 2021; 144(1):52-73.

PMID: 34078089 PMC: 8293289. DOI: 10.1161/CIRCULATIONAHA.120.047978.


ATF3 Coordinates Antitumor Synergy between Epigenetic Drugs and Protein Disulfide Isomerase Inhibitors.

Duncan R, Reyes L, Moats K, Robinson R, Murphy S, Kaur B Cancer Res. 2020; 80(16):3279-3291.

PMID: 32561529 PMC: 7442646. DOI: 10.1158/0008-5472.CAN-19-4046.