HDAC inhibitors: Targets for tumor therapy, immune
2022年2月1日 · HDAC inhibitors are emerging as a successful epigenetic therapy by exploiting pathophysiology of tumor microenvironment. HDAC inhibitors can activate multiple antitumor …
Histone deacetylase inhibitors: molecular mechanisms of action …
Histone deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell …
Histone deacetylase inhibitor - Wikipedia
Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases. Since deacetylation of histones produces transcriptionally …
Histone Deacetylase Inhibitors as Anticancer Drugs - PMC
Modification of histones by acetylation plays a key role in epigenetic regulation of gene expression and is controlled by the balance between histone deacetylases (HDAC) and histone …
Targeting the E2F1/Rb/HDAC1 axis with the small molecule …
2023年12月7日 · Histone deacetylase inhibitors (HDACis) have gradually become powerful anti-cancer agents targeting epigenetic modulation and have been widely used in the clinical …
HDAC Inhibitors: Innovative Strategies for Their Design and ...
Fluorescent deacetylase in vitro assay with a purified ternary LSD1-CoREST-HDAC1 complex proved HDAC1 inhibitory properties of all the synthesized compounds. Those with C6-linker, …
Overview of class I HDAC modulators: Inhibitors and degraders
2024年10月5日 · By connecting substituted anilines with GABA and PABA molecules, and further fusing them with 1,2-phenylenediamine, a series of novel phenyl-containing HDAC1 inhibitors …
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight
2020年7月1日 · It is now 30 years since the first report of a potent zinc-dependent histone deacetylase (HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received …
Recent Progress in Histone Deacetylase (HDAC) 1 Inhibitors as ...
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. …
Therapeutic application of histone deacetylase inhibitors for …
The benzamide inhibitor MS275 preferentially inhibits HDAC1 (IC 50 ∼ 0.3 μM) versus HDAC3 (IC 50 ∼ 8 μM); shows no inhibitory activity against HDAC8 (IC 50 >100 μM); and...