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   Articles with "hdac6" as a keyword



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Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors

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recommendations! Published in 2020 at "Chemmedchem"

DOI: 10.1002/cmdc.202000149

Abstract: We report the synthesis and evaluation of a class of selective multitarget agents for the inhibition of HDAC6, HDAC8, and HDAC10. The concept for this study grew out of a structural analysis of the two… read more here.

Keywords: design synthesis; hdac6 inhibitors; dihydroxamic acids; synthesis dihydroxamic ... See more keywords
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Developing potent PROTACs tools for selective degradation of HDAC6 protein

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recommendations! Published in 2019 at "Protein & Cell"

DOI: 10.1007/s13238-018-0602-z

Abstract: Histone deacetylases (HDACs) are a family of enzymes that remove acetyl groups on histone and non-histone proteins, thereby playing a vital role in the modulation of gene expression and protein activity. Eighteen HDACs have been… read more here.

Keywords: degradation; protacs; hdac6; cell ... See more keywords

HDAC6 deficiency induces apoptosis in mesenchymal stem cells through p53 K120 acetylation.

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recommendations! Published in 2017 at "Biochemical and biophysical research communications"

DOI: 10.1016/j.bbrc.2017.10.087

Abstract: The acetylation of p53 is critical in modulating its pro-apoptotic roles. However, its regulatory mechanism and physiological significance are unclear. Here, we show HDAC6 negatively regulates pro-apoptotic acetylation of p53 at lysine residue 120 (K120) in… read more here.

Keywords: acetylation; k120 acetylation; hdac6; p53 ... See more keywords
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Discovery of specific HDAC6 inhibitor with anti-metastatic effects in pancreatic cancer cells through virtual screening and biological evaluation.

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recommendations! Published in 2020 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2020.103679

Abstract: Histone deacetylase 6 (HDAC6) has been demonstrated to play a major role in cell motility and aggresome formation, and HDAC6 inhibition is therefore considered as a promising epigenetic strategy for cancer treatment. At present, only… read more here.

Keywords: virtual screening; hdac6 inhibitors; cefoperazone sodium; cancer ... See more keywords
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Novel pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione (PBD) derivatives as selective HDAC6 inhibitors to suppress tumor metastasis and invasion in vitro and in vivo.

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recommendations! Published in 2021 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2021.105081

Abstract: Selective inhibition of histone deacetylase 6 (HDAC6) has been emerged as a promising approach to cancer treatment. As a pivotal strategy for drug discovery,molecular hybridization was introduced in this study and a series of pyrrolo[2,1-c][1,4]… read more here.

Keywords: hdac6 inhibitors; vitro vivo; metastasis; selective hdac6 ... See more keywords
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MAP3K4 Controls the Chromatin Modifier HDAC6 during Trophoblast Stem Cell Epithelial-to-Mesenchymal Transition.

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recommendations! Published in 2017 at "Cell reports"

DOI: 10.1016/j.celrep.2017.02.030

Abstract: The first epithelial-to-mesenchymal transition (EMT) occurs in trophoblast stem (TS) cells during implantation. Inactivation of the serine/threonine kinase MAP3K4 in TS cells (TSKI4 cells) induces an intermediate state of EMT, where cells retain stemness, lose… read more here.

Keywords: mesenchymal transition; map3k4; epithelial mesenchymal; hdac6 ... See more keywords
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HDAC6 Suppresses Age-Dependent Ectopic Fat Accumulation by Maintaining the Proteostasis of PLIN2 in Drosophila.

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recommendations! Published in 2017 at "Developmental cell"

DOI: 10.1016/j.devcel.2017.09.001

Abstract: Age-dependent ectopic fat accumulation (EFA) in animals contributes to the progression of tissue aging and diseases such as obesity, diabetes, and cancer. However, the primary causes of age-dependent EFA remain largely elusive. Here, we characterize… read more here.

Keywords: age dependent; age; proteostasis; plin2 ... See more keywords
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TLR4-TAK1-p38 MAPK pathway and HDAC6 regulate the expression of sigma-1 receptors in rat primary cultured microglia.

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recommendations! Published in 2020 at "Journal of pharmacological sciences"

DOI: 10.1016/j.jphs.2020.06.007

Abstract: Microglia maintain brain homeostasis as the main immune cells in the central nervous system. Activation of sigma-1 receptor (Sig1R) plays neuroprotective and anti-inflammatory roles in microglia. Recent studies showed that Sig1R expression level has been… read more here.

Keywords: sig1r; tak1 p38; expression; hdac6 ... See more keywords
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HDAC6 as privileged target in drug discovery: A perspective.

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recommendations! Published in 2020 at "Pharmacological research"

DOI: 10.1016/j.phrs.2020.105274

Abstract: HDAC6, a class II b HDAC isoenzyme, stands unique in its structural and physiological functions. Besides histone modification, largely due to its cytoplasmic localization, HDAC6 also targets several non-histone proteins including Hsp90, α-tubulin, cortactin, HSF1,… read more here.

Keywords: privileged target; discovery perspective; target drug; hdac6 ... See more keywords
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Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.

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recommendations! Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c01659

Abstract: In this work, we utilized the proteolysis targeting chimera (PROTAC) technology to achieve the chemical knock-down of histone deacetylase 6 (HDAC6). Two series of cereblon-recruiting PROTACs were synthesized via a solid-phase parallel synthesis approach, which… read more here.

Keywords: solid phase; hdac6; cereblon recruiting; histone deacetylase ... See more keywords
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Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity.

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recommendations! Published in 2017 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.6b00124

Abstract: Histone deacetylase (HDAC) proteins are epigenetic regulators that deacetylate protein substrates, leading to subsequent changes in cell function. HDAC proteins are implicated in cancers, and several HDAC inhibitors have been approved by the FDA as… read more here.

Keywords: saha analogues; position; hdac inhibitors; hdac6 ... See more keywords