Exploring the binding mechanism of HDAC8 selective inhibitors: Lessons from the modification of Cap group
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.29583
Abstract: The abnormal expression of histone deacetylase 8 (HDAC8) has been reported to associate with various cancer entities (colon, breast cancer, pancreas, etc.) as well as parasitic diseases, making HDAC8 gradually develop into an attractive and… read more here.
Keywords: binding mechanism; hdac8; group; modification cap ... See more keywords
HDAC8 regulates canonical Wnt pathway to promote differentiation in skeletal muscles
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular Physiology"
DOI: 10.1002/jcp.27341
Abstract: Histone deacetylase 8 (HDAC8) is a class 1 histone deacetylase and a member of the cohesin complex. HDAC8 is expressed in smooth muscles, but its expression in skeletal muscle has not been described. We have… read more here.
Keywords: muscle; hdac8; canonical wnt; skeletal muscles ... See more keywords
Histone deacetylase 8 (HDAC8) and its inhibitors with selectivity to other isoforms: An overview.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.12.039
Abstract: The histone deacetylases (HDACs) enzymes provided crucial role in transcriptional regulation of cells through deacetylation of nuclear histone proteins. Discoveries related to the HDAC8 enzyme activity signified the importance of HDAC8 isoform in cell proliferation,… read more here.
Keywords: inhibitors selectivity; hdac8 inhibitors; hdac8; histone deacetylase ... See more keywords
Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01025
Abstract: HDACs are an attractive therapeutic target for a variety of human diseases. Currently, all four FDA-approved HDAC-targeting drugs are non-selective, pan-HDAC inhibitors, exhibiting adverse side-effects at therapeutic doses. While selective HDAC-inhibition has been proposed to… read more here.
Keywords: conformationally constrained; hdac8; benzanilide scaffolds; scaffolds potent ... See more keywords
Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00761
Abstract: HDAC8 plays crucial roles in biological processes, from gene regulation to cell motility, making it a highly desirable target for therapeutic intervention. HDAC8 also has deacetylase-independent activity which cannot be blocked by a conventional inhibitor.… read more here.
Keywords: hdac8 degrader; potent selective; highly potent; degrader ... See more keywords
Natural Derivatives of Selective HDAC8 Inhibitors with Potent in Vivo Antitumor Efficacy against Breast Cancer.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c01438
Abstract: HDAC8 is a therapeutic target with great promise for breast cancer. Here, we reported a novel compound corallorazine D from Nocardiopsis sp. XZB108, selectively inhibited HDAC8 (IC50 = 0.90 ± 0.014 μM), suggesting that it… read more here.
Keywords: antitumor; efficacy; breast cancer; hdac8 ... See more keywords
Structure-Based Design and Biological Characterization of Selective Histone Deacetylase 8 (HDAC8) Inhibitors with Anti-Neuroblastoma Activity.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01447
Abstract: Histone deacetylases (HDACs) are important modulators of epigenetic gene regulation and additionally control the activity of non-histone protein substrates. While for HDACs 1-3 and 6 many potent selective inhibitors have been obtained, for other subtypes… read more here.
Keywords: hdac8 inhibitors; hdac8; activity; structure based ... See more keywords
HDAC8 promotes the dissemination of breast cancer cells via AKT/GSK-3β/Snail signals
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DOI: 10.1038/s41388-020-1337-x
Abstract: The mechanistic action of histone deacetylase 8 (HDAC8) in cancer motility, including epithelial-mesenchymal transition (EMT), remains largely undefined. We found that the expression of HDAC8 was upregulated in breast cancer (BC) cells and tissues as… read more here.
Keywords: hdac8; breast cancer; snail; cancer cells ... See more keywords
Discovery of novel potential selective HDAC8 inhibitors by combine ligand-based, structure-based virtual screening and in-vitro biological evaluation
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-53376-y
Abstract: Neuroblastoma is the most common extracranial solid tumor found in children and survival rate is extremely meager. HDAC8, a class I zinc-dependent enzyme, is a potential drug target for treatment of neuroblastoma and T cell… read more here.
Keywords: virtual screening; novel potential; hdac8 inhibitors; hdac8 ... See more keywords
Epigenetic-based cancer therapeutics: new potential HDAC8 inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2020.1813203
Abstract: Abstract Designing dual small molecule inhibitors against enzymes associated with cancer has turned into a new strategy in cancer chemotherapy. Targeting DNA methyltransferase (DNMT) and histone deacetylase (HDAC) enzymes, involved in epigenetic modifications, are considered… read more here.
Keywords: cancer; therapeutics new; cancer therapeutics; hdac8 ... See more keywords
HDAC8 Promotes Liver Metastasis of Colorectal Cancer via Inhibition of IRF1 and Upregulation of SUCNR1
Sign Up to like & getrecommendations! Published in 2022 at "Oxidative Medicine and Cellular Longevity"
DOI: 10.1155/2022/2815187
Abstract: Histone deacetylases (HDACs) are well-characterized for their involvement in tumor progression. Herein, the current study set out to unravel the association of HDAC8 with colorectal cancer (CRC). Bioinformatics analyses were carried out to retrieve the… read more here.
Keywords: hdac8; cell; sucnr1; crc ... See more keywords