HDAC inhibitor ameliorates behavioral deficits in Mecp2 308/y mouse model of Rett syndrome
Sign Up to like & getrecommendations! Published in 2021 at "Brain Research"
DOI: 10.1016/j.brainres.2021.147670
Abstract: Rett syndrome (RTT) is a rare X-linked neurodevelopmental disorder. More than 95% of classic RETT syndrome cases result from pathogenic variants in the methyl-CpG binding protein 2 (MECP2) gene. Nevertheless, it has been established that… read more here.
Keywords: inhibitor ameliorates; rett syndrome; mecp2 308; mecp2 deficient ... See more keywords
Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.12.047
Abstract: HDAC inhibitors and NO donors have already revealed independently their broad therapeutic potential in pathologic contexts. Here we further investigated the power of their combination in a single hybrid molecule. Nitrooxy groups or substituted furoxan… read more here.
Keywords: structural biological; biological characterization; hdac; new hybrid ... See more keywords
Potential repurposing of the HDAC inhibitor valproic acid for patients with COVID-19
Sign Up to like & getrecommendations! Published in 2021 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2021.173988
Abstract: There is a need for therapeutic approaches to prevent and mitigate the effects of Coronavirus Disease 2019 (COVID-19). The histone deacetylase (HDAC) inhibitor valproic acid, which has been available for the therapy of epilepsy for… read more here.
Keywords: hdac inhibitor; acid; inhibitor valproic; valproic acid ... See more keywords
HDAC inhibitor affects soybean miRNA482bd expression under salt and osmotic stress.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of plant physiology"
DOI: 10.1016/j.jplph.2020.153261
Abstract: MicroRNAs (miRNAs) are small non-coding molecules that modulate gene expression through targeting mRNA by specific-sequence cleavage, translation inhibition, or transcriptional regulation. miRNAs are key molecules in regulatory networks in abiotic stresses such as salt stress… read more here.
Keywords: salt stress; stress; expression; hdac inhibitor ... See more keywords
Unexpected Biotransformation of the HDAC Inhibitor Vorinostat Yields Aniline-Containing Fungal Metabolites.
Sign Up to like & getrecommendations! Published in 2017 at "ACS chemical biology"
DOI: 10.1021/acschembio.7b00268
Abstract: The diversity of genetically encoded small molecules produced by filamentous fungi remains largely unexplored, which makes these fungi an attractive source for the discovery of new compounds. However, accessing their full chemical repertoire under common… read more here.
Keywords: aniline containing; vorinostat; inhibitor vorinostat; hdac inhibitor ... See more keywords
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00014
Abstract: Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)micromolar inhibition against both targets. When tested in several cancer cell… read more here.
Keywords: class dual; dual ezh2; ezh2 hdac; hdac inhibitor ... See more keywords
The first-in-class alkylating HDAC inhibitor EDO-S101 is highly synergistic with proteasome inhibition against multiple myeloma through activation of multiple pathways
Sign Up to like & getrecommendations! Published in 2017 at "Blood Cancer Journal"
DOI: 10.1038/bcj.2017.69
Abstract: The first-in-class alkylating HDAC inhibitor EDO-S101 is highly synergistic with proteasome inhibition against multiple myeloma through activation of multiple pathways read more here.
Keywords: alkylating hdac; edo s101; inhibitor edo; class alkylating ... See more keywords
Elucidation of the working principle of a gene-directed caged HDAC inhibitor with cell-type selectivity.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc03552a
Abstract: Histone deacetylases (HDACs) play crucial roles in the epigenetic regulation of gene expression. Here, we report CM-Bhc-SAHA, a novel caged HDAC inhibitor, genetically targeting cells of interest. Mammalian cells expressing porcine liver esterase led to… read more here.
Keywords: gene; hdac inhibitor; caged hdac; elucidation working ... See more keywords
HDAC inhibitor, MS-275, increases vascular permeability by suppressing Robo4 expression in endothelial cells
Sign Up to like & getrecommendations! Published in 2021 at "Tissue Barriers"
DOI: 10.1080/21688370.2021.1911195
Abstract: ABSTRACT Roundabout guidance receptor 4 (Robo4) is an endothelial-specific membrane protein that suppresses pathological angiogenesis and vascular hyperpermeability by stabilizing endothelial cells. Robo4 suppresses severe systemic inflammation induced by pathogens and endotoxins and inhibits tumor… read more here.
Keywords: robo4 expression; expression; endothelial cells; hdac inhibitor ... See more keywords
DIPG-71. SELECTIVE HDAC INHIBITOR RG2833 INDUCES DIPG CELL DEATH VIA DOWNREGULATION OF THE NFĸB PATHWAY
Sign Up to like & getrecommendations! Published in 2020 at "Neuro-Oncology"
DOI: 10.1093/neuonc/noaa222.113
Abstract: Abstract Histone deacetylase (HDAC) inhibitor panobinostat demonstrated activity against diffuse intrinsic pontine glioma (DIPG) in vitro, but its efficacy in vivo was limited by toxicity and poor blood brain barrier penetration. RG2833 (RGFP109) is a… read more here.
Keywords: hdac inhibitor; rg2833; dipg cell; dmso ... See more keywords
Upregulation of C/EBPβ and TSC2 by an HDAC inhibitor CG200745 protects heart from DOCA‐induced hypertrophy
Sign Up to like & getrecommendations! Published in 2019 at "Clinical and Experimental Pharmacology and Physiology"
DOI: 10.1111/1440-1681.13022
Abstract: Histone deacetylases (HDACs) are a vast family divided into four major classes: class I (1, 2, 3, and 8), class II (4, 5, 6, 7, 9 and 10), class III (sirtuin family) and class IV… read more here.
Keywords: hypertrophy; ebp tsc2; tsc2; hdac inhibitor ... See more keywords