Title:Recent Progress in Histone Deacetylase (HDAC) 1 Inhibitors as Anticancer
Agent
Volume: 23
Issue: 1
Author(s): Preeti Patel*, Simranpreet K. Wahan, S. Vishakha, Balak Das Kurmi, Ghanshyam Das Gupta, Harish Rajak and Vivek Asati
Affiliation:
- Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga-142001, Punjab, India
Keywords:
Histone deacetylases 1(HDAC1), anticancer, hydroxamic acid derivatives, benzamides, hydrazides, thiols.
Abstract: Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing histone
deacetylation. Aberrant expression of HDACs is associated with various human diseases. Although
HDAC inhibitors are used as effective chemotherapeutic agents in clinical practice, their applications
remain limited due to associated side effects induced by weak isoform selectivity. HDAC1 displays
unique structure and cellular localization as well as diverse substrates and exhibits a wider range of biological
functions than other isoforms. HDAC1 displays a unique structure primarily found in the nucleus
and involved in epigenetic and transcriptional regulation. HDAC1 is ubiquitously expressed and associated
with Sin3, NuRD, and CoRest transcription repressive complexes responsible for distinct cellular
processes like cell proliferation and survival. HDAC1 inhibitors have been effectively used to treat
various cancers such as gastric, breast, colorectal, prostate, colon, lung, ovarian, pancreatic, and inflammation
without exerting significant toxic effects. In this review, we summarize four major structural
classes of HDAC1 inhibitors (i.e., hydroxamic acid derivatives, benzamides, hydrazides, and thiols)
with their structural activity relationship. This review is a comprehensive work on HDAC1 inhibitors to
achieve deep insight of knowledge about the structural information of HDAC1 inhibitors. It may provide
up-to-date direction for developing new selective HDAC1 inhibitors as anticancer agents.