Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 178, Issue -, Pages 259-286Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.05.078
Keywords
Epigenetics; Histone acetyltransferase inhibitors; Drug design; Drug synthesis; Structure-activity relationship
Categories
Funding
- National Natural Science Foundation of China [21702141]
- China Postdoctoral Science Foundation [2017M623050]
- Sichuan University [2017SCU12061]
Ask authors/readers for more resources
Acetylation, a key component in post-translational modification regulated by HATS and HDACs, is relevant to many crucial cellular contexts in organisms. Based on crucial pharmacophore patterns and the structure of targeted proteins, HAT inhibitors are designed and modified for higher affinity and better bioactivity. However, there are still some challenges, such as cell permeability, selectivity, toxicity and synthetic availability, which limit the improvement of HAT inhibitors. So far, only few HAT inhibitors have been approved for commercialization, indicating the urgent need for more successful and effective structure-based drug design and synthetic strategies. Here, we summarized three classes of HAT inhibitors based on their sources and structural scaffolds, emphasizing on their synthetic methods and structure activity relationships and molecular mechanisms, hoping to facilitate the development and further application of HAT inhibitors. (C) 2019 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available