Histone deacetylase (HDAC) inhibition is a process in which enzymes that normally remove acetyl groups from histones are blocked. Histones are proteins that form part of the structure of chromosomes, and their acetylation or deacetylation affects several cellular processes, including gene expression, DNA repair, and cell differentiation. Inhibition of HDACs increases the level of histone acetylation, which has been shown to have a wide range of effects on gene expression and cellular function. HDAC inhibitors are being studied as potential treatments for a variety of diseases, including cancer, neurodegenerative disorders, and autoimmune diseases.
HDAC inhibition can counteract the abnormal acetylation status of proteins found in cancer cells and can reactivate the expression of tumor suppressors {ref}
Phenylbutyrate is a prodrug that is metabolized to phenylacetate, which is the active molecule that combines with glutamine (an amino acid with two nitrogen molecules) to form phenylacetylglutamine which is rapidly excreted by the kidneys and does not require metabolism via the urea cycle. Phenylbutyrate thus provides an “ammonia sink”, an alternative pathway for excretion of excess nitrogen and ammonia Ref
- Peptides {review}
- Antineoplastons A10 and AS2-1
- Cyproheptadine, an anti-histaminic, synergizes the antineoplastic activity of bortezomib in mantle cell lymphoma through its effects as a histone deacetylase inhibitor. {study}
cyproheptadine demonstrated activity in in vitro and in vivo models of MCL with a mechanism of action resembling a classic HDACI
- L-carnitine {ref}
- Curcumin can decrease the expression of HDAC1, HDAC3 and HDAC8 by increasing the acetylated level of histone H4 {study}
- Butyrate 🛈 decreases its own oxidation in colorectal cancer cells through inhibition of histone deacetylases
- Diallyl disulfide can inhibit cell proliferation through the inhibition of HDAC activity, histone hyperacetylation and increase in p21(waf1/cip1) expression.{study}
- Luteolin Causes 5'CpG Demethylation of the Promoters of TSGs and Modulates the Aberrant Histone Modifications, Restoring the Expression of TSGs in Human Cancer Cells
- Sulforaphane
- Trichostatin A
- Melatonin 🛈
- Niacin
- + PDL1i 🛈
Natural Bioactive Compounds Targeting Histone Deacetylases in Human Cancers: Recent Updates
Examples of dietary compounds that regulate histone acetylation.
Books
- Fighting Cancer Through HDAC and MAPK Inhibitors by Anna Purna Edara
- Histone Deacetylase Inhibitors in Combinatorial Anticancer Therapy by Ganai, Shabir Ahmad
Illustrations
 |
| https://www.mdpi.com/2073-4409/8/8/930 |
.jpeg)
No comments:
Post a Comment