Journal
CHEMMEDCHEM
Volume 14, Issue 11, Pages 1067-1073Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201900174
Keywords
Alzheimer's disease; drug design; histone deacetylase inhibitors; multitarget ligands; neuroprotection
Categories
Funding
- University of Bologna (RFO)
Ask authors/readers for more resources
Histone deacetylase inhibitors (HDACIs) are responsible for controlling gene expression by modulating the acetylation status of histone proteins. Furthermore, they modulate the activity of cytoplasmic non-histone proteins. Due to the involvement of HDACs in neurodevelopment, memory formation, and cognitive processes, HDACIs have been suggested as innovative agents for the treatment of neurodegenerative disorders such as Alzheimer's disease (AD). Given their mechanisms of action and the complex nature of AD, HDACIs have been proposed for the design of novel multitarget ligands (MTLs). To this aim, the fragment responsible for HDAC inhibition has been coupled with other structures that are able to provide additional biological actions, such as antioxidant activity or the inhibition of phosphodiesterase 5, transglutaminase 2, and glycogen synthase kinase 3 beta. Herein we discuss recent efforts to design HDACI-based MTLs as potential disease-modifying entities.
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