Balancing Histone Deacetylase (HDAC) Inhibition and Drug‐likeness: Biological and Physicochemical Evaluation of Class I Selective HDAC Inhibitors
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DOI: 10.1002/cmdc.202100755
Abstract: Herein we report the structure‐activity and structure‐physicochemical property relationships of a series of class I selective ortho‐aminoanilides targeting the “foot‐pocket” in HDAC1&2. To balance the structural benefits and the physicochemical disadvantages of these substances, we… read more here.
Keywords: evaluation; inhibition; class; balancing histone ... See more keywords
A histone deacetylase, MoHOS2 regulates asexual development and virulence in the rice blast fungus
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DOI: 10.1007/s12275-019-9363-5
Abstract: Histone acetylation/deacetylation represent a general and efficient epigenetic mechanism through which fungal cells control gene expression. Here we report developmental requirement of MoHOS2-mediated histone deacetylation (HDAC) for the rice blast fungus, Magnaporthe oryzae. Structural similarity… read more here.
Keywords: blast fungus; mohos2; rice blast; hdac ... See more keywords
In silico identification of 2-oxo-1,3-thiazolidine derivatives as novel inhibitor candidate of class II histone deacetylase (HDAC) in cervical cancer treatment
Sign Up to like & getrecommendations! Published in 2019 at "Arabian Journal of Chemistry"
DOI: 10.1016/j.arabjc.2015.07.010
Abstract: Abstract Cervical cancer ranks third among the most prevalent deadly cancer in women worldwide and ranks first in developing countries. It is caused by human papilloma virus (HPV) infection. Thus HDACs have become prominent inhibition… read more here.
Keywords: best ligands; analysis; hdac; pharmacology ... See more keywords
HDAC inhibitor suppresses proliferation and invasion of breast cancer cells through regulation of miR‐200c targeting CRKL
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DOI: 10.1016/j.bcp.2017.11.008
Abstract: ABSTRACT Although histone deacetylase (HDAC) inhibitors have been shown to effectively induce the inhibition of proliferation and migration in breast cancer, the anticancer mechanism remains poorly understood. Our studies show that miR‐200c was significantly downregulated… read more here.
Keywords: crkl; hdac; mir 200c; breast cancer ... See more keywords
Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors.
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DOI: 10.1016/j.bioorg.2022.105702
Abstract: On the basis of synergistic effect between topoisomerase (Top) and histone deacetylase (HDAC) inhibitors, a series of novel evodiamine-based Top/HDAC dual inhibitors were designed and synthesized. Systematic structure-activity relationship (SAR) studies led to the discovery… read more here.
Keywords: topoisomerase top; evodiamine based; hdac dual; dual inhibitors ... See more keywords
Structural and biological characterization of new hybrid drugs joining an HDAC inhibitor to different NO-donors.
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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
Design, synthesis, and biological evaluation of novel amide and hydrazide based thioether analogs targeting Histone deacteylase (HDAC) enzymes.
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DOI: 10.1016/j.ejmech.2018.02.011
Abstract: Development of HDAC inhibitors have become an ultimate need targeting different types of cancer. In silico virtual screening was applied to screen novel scaffolds via scaffold hopping strategy to develop different acrylamide and aryl/heteroaryl hydrazide… read more here.
Keywords: hydrazide based; cell lines; based analogs; hdac ... See more keywords
Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
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DOI: 10.1016/j.ejmech.2021.113338
Abstract: Hurdled and marred by the notorious nature of glioblastomas (GBM) in terms of resistance to therapy and limited drug delivery into the brain, the anti-GBM drug pipeline is required to be loaded with mechanistically diverse… read more here.
Keywords: gbm; group; hdac inhibitors; gbm cells ... See more keywords
Identification of novel class I and class IIb histone deacetylase inhibitor for Alzheimer's disease therapeutics.
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DOI: 10.1016/j.lfs.2020.117912
Abstract: Histone deacetylase enzymes were prominent chromatin remodeling drug that targets in the pathophysiology of Alzheimer's disease associated with transcriptional dysregulation. In vitro and in vivo models of AD have demonstrated overexpression of HDAC activity. Non-specificity… read more here.
Keywords: class iib; inhibitor; class; hdac ... See more keywords
Manganese chloride induces histone acetylation changes in neuronal cells: Its role in manganese‐induced damage
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DOI: 10.1016/j.neuro.2017.11.003
Abstract: Graphical abstract Manganese chloride may inhibit the acetylation of histone H3 and H4 by increasing the activity of HDAC, and decreasing that of HAT, which finally caused the cell damage and apoptosis in neuronal cells.… read more here.
Keywords: manganese chloride; histone acetylation; neuronal cells; acetylation ... See more keywords
Histone deacetylases in cardiovascular and metabolic diseases.
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DOI: 10.1016/j.yjmcc.2019.04.003
Abstract: Histone deacetylases (HDACs) regulate gene transcription by catalyzing the removal of acetyl groups from key lysine residues in nucleosomal histones and via the recruitment of other epigenetic regulators to DNA promoter/enhancer regions. Over the past… read more here.
Keywords: cardiovascular metabolic; metabolic diseases; histone deacetylases; deacetylases cardiovascular ... See more keywords