Advances in histone epigenetic enzyme inhibitors based on proteomics
10.16438/j.0513-4870.2022-0937
- VernacularTitle:基于蛋白质组学的组蛋白表观遗传酶抑制剂研究进展
- Author:
Quan LIU
1
;
Lu-lu WANG
2
;
Jun-yu XU
3
;
Min-jia TAN
4
Author Information
1. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China
2. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China; School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
3. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China
4. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China; School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
- Publication Type:Research Article
- Keywords:
proteomics;
histone modification;
histone methyltransferase;
histone deacetylase;
epigenetic inhibitor
- From:
Acta Pharmaceutica Sinica
2023;58(9):2541-2550
- CountryChina
- Language:Chinese
-
Abstract:
As an important component of nucleosomes on the chromatin of eukaryotic cells, histones play an important role in the development and progression of tumour diseases by regulating epigenetic post-translational modifications such as acetylation and methylation. In addition, development of inhibitors targeting methyltransferase and deacetylase provides novel therapeutic strategies for cancer treatment. Mass spectrometry-based proteomics can reveal the global changes of histone modifications under the action of drugs during disease progression, which in turn provides important support for revealing drug action mechanism, drug resistance mechanism, and investigating novel drug combination strategies. This article focuses on the progress and status of proteomic research on a variety of histone modifying enzyme inhibitors, including methyltransferase inhibitors and histone deacetylase inhibitors, which will help to understand the current and further utilization of proteomics in studying histone modifications.
