Search results for "Histone"

showing 10 items of 522 documents

Induction of Apoptosis and Chemosensitization by the Histone Deacetylase Inhibitor Trichostatin in Hepatocellular Carcinoma Cells: Molecular Analysis…

2011

The mRNA and protein levels of RKIP are reduced and those of YY1 increased in clinical HCC. Loss, mutation, or promoter hypermethylation of the RKIP gene may not account for the downregulation of RKIP in HCC. Histone deacetylation can silence gene expression and play a significant role in hepatocarcinogenesis. The histone deacetylase inhibitor (HDACI) trichostatin induced cell growth inhibition and proapoptotic effects in HA22T/VGH and HepG2 HCC cells; it also exhibited synergy with doxorubicin. Treatment with trichostatin caused histone hyperacetylation and down- or upregulated expression of different genes (such as β-catenin, cyclin D1, hTERT, XIAP, and IL-6). These changes might, at leas…

hepatocellular carcinoma Raf-1 kinase inhibitor protein Yin Yang 1 gene expression histone deacetylase inhibitor trichostatin apoptosis chemosensitizationHistone deacetylase 5medicine.drug_classChemistryHDAC11Histone deacetylase inhibitormedicine.diseaseBiochemistryMolecular biologyMolecular analysisApoptosisChemosensitizationHepatocellular carcinomaGene expressionGeneticsmedicineCancer researchSettore BIO/14 - FarmacologiaMolecular MedicineBiotechnology
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Effetto citotossico di un nuovo inibitore delle deacetilasi istoniche, JAHA, su cellule di tumore mammario umano triplo negativo

2013

histone deacetylase inhibitor breast cancer cytotoxicitySettore BIO/06 - Anatomia Comparata E Citologia
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Cytotoxic effects induced by JA47, a novel histone deacetylase inhibitor (HDACi), on MDA-MB231 breast cancer cells

2012

histone deacetylase inhibitor breast cancer cytotoxicitySettore BIO/06 - Anatomia Comparata E Citologia
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JA47, a new histone deacetylase inhibitor that induces cytotoxic effects on triple-negative MDA-MB231 breast cancer cells in vitro

2012

histone deacetylase inhibitor cytotoxicity breast cancer cells autophagy reactive oxygen species cell cycleSettore BIO/06 - Anatomia Comparata E Citologia
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Biological effect of an hybrid anticancer agent based on kinase and histone deacetylase inhibitor on breast cancer cells

2014

histone deacetylase inhibitor hybrid drug breast cancer cellsSettore BIO/06 - Anatomia Comparata E Citologia
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Hydroxamic acid-containing histone deacetylase inhibitors potentiate the antiproliferative and apoptotic effects induced by the ribonucleotide reduct…

2008

histone deacetylase inhibitors ribonucleotide reductase inhibitors cell cycle
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Rat PIPPin is probably part of a large complex of RNA-binding proteins

2012

Throughout rat brain development, expression of histones variants is mainly regulated at the post-transcriptional level. We previously cloned two cDNAs encoding, respectively, PIPPin (or CSD-C2), a brain-enriched protein able to bind the 3’end of H1° and H3.3 mRNAs, and LPI (longer isoform of PEP-19). Both PEP-19 and LPI are brain-specific. By western blot, we found that PIPPin expression in PC12 cells is enhanced by NGF-induced differentiation. We investigated the RNA-binding properties of the three proteins using their 6 histidine-tagged recombinant fusions and found that they all bind H1° and H3.3 RNAs. Since PEP-19 and LPI are camstatins, we also analyzed whether calmodulin could interf…

histone variantPIPPinRBPSettore BIO/10 - BiochimicaLPISettore BIO/06 - Anatomia Comparata E CitologiaCSD-C2hnRNP
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Role of RNA-binding proteins in the replication-independent expression of H1° and H3.3 histone variants

2012

histone variantRNA-binding proteinSettore BIO/10 - BiochimicaLPISettore BIO/06 - Anatomia Comparata E CitologiaCSD-C2PEP-19
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Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.

2021

Quinoline is one of the most important and versatile nitrogen heterocycles embodied in several biologically active molecules. Within the numerous quinolines developed as antiproliferative agents, this review is focused on compounds interfering with DNA structure or with proteins/enzymes involved in the regulation of double helix functional processes. In this light, a special focus is given to the quinoline compounds, acting with classical/well-known mechanisms of action (DNA intercalators or Topoisomerase inhibitors). In particular, the quinoline drugs amsacrine and camptothecin (CPT) have been studied as key lead compounds for the development of new agents with improved PK and tolerability…

medicine.drug_classAntineoplastic Agents01 natural sciences03 medical and health scienceschemistry.chemical_compoundDrug DiscoverymedicineHumansAmsacrine030304 developmental biologyCell ProliferationPharmacology0303 health sciencesDNA Intercalators G-quadruplex Topoisomerase Epigenetic targets Antiproliferative compounds SAR studiesbiologyMolecular Structure010405 organic chemistryTopoisomeraseOrganic ChemistryQuinolineGeneral MedicineDNA NeoplasmSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesDNA-Binding ProteinsG-QuadruplexesHistonechemistryBiochemistrybiology.proteinQuinolinesHistone deacetylaseCamptothecinDNATopoisomerase inhibitormedicine.drugEuropean journal of medicinal chemistry
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Cytotoxic effects of Jay Amin hydroxamic acid (JAHA), a ferrocene-based class I histone deacetylase inhibitor, on triple-negative MDA-MB231 breast ca…

2012

The histone deacetylase inhibitors (HDACis) are a class of chemically heterogeneous anticancer agents of which suberoylanilide hydroxamic acid (SAHA) is a prototypical member. SAHA derivatives may be obtained by three-dimensional manipulation of SAHA aryl cap, such as the incorporation of a ferrocene unit like that present in Jay Amin hydroxamic acid (JAHA) and homo-JAHA [ Spencer , et al. ( 2011 ) ACS Med. Chem. Lett. 2 , 358 - 362 ]. These metal-based SAHA analogues have been tested for their cytotoxic activity toward triple-negative MDA-MB231 breast cancer cells. The results obtained indicate that of the two compounds tested, only JAHA was prominently active on breast cancer cells with a…

medicine.drug_classCell SurvivalMetallocenesAntineoplastic AgentsApoptosisToxicologyHydroxamic AcidsStructure-Activity RelationshipIn vivoAnnexinmedicineTumor Cells CulturedCytotoxic T cellHumansFerrous CompoundsSettore BIO/06 - Anatomia Comparata E Citologiachemistry.chemical_classificationMembrane Potential MitochondrialReactive oxygen speciesDose-Response Relationship DrugMolecular StructureChemistryHistone deacetylase inhibitorCell CycleGeneral MedicineIn vitroHistone Deacetylase InhibitorsBiochemistryhistone deacetylase inhibitor breast cancer autophagy apoptosis mitochondria cell cycleApoptosisCancer researchHistone deacetylaseDrug Screening Assays AntitumorReactive Oxygen Species
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