0000000000791646

AUTHOR

Lucia Altucci

showing 3 related works from this author

Combined HAT/EZH2 modulation leads to cancer-selective cell death

2018

Contains fulltext : 197351.pdf (Publisher’s version ) (Open Access) Epigenetic alterations have been associated with both pathogenesis and progression of cancer. By screening of library compounds, we identified a novel hybrid epi-drug MC2884, a HAT/EZH2 inhibitor, able to induce bona fide cancer-selective cell death in both solid and hematological cancers in vitro, ex vivo and in vivo xenograft models. Anticancer action was due to an epigenome modulation by H3K27me3, H3K27ac, H3K9/14ac decrease, and to caspase-dependent apoptosis induction. MC2884 triggered mitochondrial pathway apoptosis by up-regulation of cleaved-BID, and strong down-regulation of BCL2. Even aggressive models of cancer, …

0301 basic medicineacetylation; apoptosis; cancer; epigenetics; methylation; oncologyProgrammed cell death[SDV.CAN]Life Sciences [q-bio]/Cancer03 medical and health sciencesacetylation; apoptosis; cancer; epigenetics; methylationIn vivomedicinecancerMolecular Biologyacetylationepigeneticsbusiness.industryCancer; Epigenetics; Apoptosis; Acetylation; MethylationEZH2apoptosisApoptosiEpigeneticCancerEpigenomemedicine.disease3. Good healthLeukemia030104 developmental biologyOncologyApoptosisCancer researchmethylationbusinessEx vivoResearch PaperOncotarget
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Essential versus accessory aspects of cell death: recommendations of the NCCD 2015

2015

Cells exposed to extreme physicochemical or mechanical stimuli die in an uncontrollable manner, as a result of their immediate structural breakdown. Such an unavoidable variant of cellular demise is generally referred to as ?accidental cell death' (ACD). In most settings, however, cell death is initiated by a genetically encoded apparatus, correlating with the fact that its course can be altered by pharmacologic or genetic interventions. "Regulated cell death" (RCD) can occur as part of physiologic programs or can be activated once adaptive responses to perturbations of the extracellular or intracellular microenvironment fail. The biochemical phenomena that accompany RCD may be harnessed to…

Biochemical Manifestations of Cell DeathISCHEMIA-REPERFUSION INJURYApoptosisReviewTransduction (genetics)0302 clinical medicineCASPASE INHIBITION SWITCHESAnimals; Humans; Terminology as Topic; Apoptosis; Signal Transduction610 Medicine & healthCaspaseTUMOR-NECROSIS-FACTOR0303 health sciencesSettore BIO/17biologySettore BIO/11NeurodegenerationSettore BIO/13APOPTOSIS3. Good healthMedicina Básicacell death030220 oncology & carcinogenesiscell death; Morphologic Aspects of Cell Death; Biochemical Manifestations of Cell DeathSignal transductionDOMAIN-LIKE PROTEINIntracellularHumanSignal TransductionNecroptosiCYTOCHROME-C RELEASEOUTER-MEMBRANE PERMEABILIZATIONProgrammed cell deathCIENCIAS MÉDICAS Y DE LA SALUDSettore BIO/06Inmunología610 Medicine & healthCELL DEATHNOQ-VD-OPH03 medical and health sciencesSettore MED/04 - PATOLOGIA GENERALEddc:570Terminology as TopicAPOPTOSIS-INDUCING FACTORMIXED LINEAGE KINASEmedicineAnimalsHumansAnimals; Humans; Terminology as Topic; Apoptosis; Signal Transduction; Molecular Biology; Cell BiologyMorphologic Aspects of Cell DeathSettore BIO/10Molecular Biology030304 developmental biologyAnimalCell growthApoptosiBiology and Life SciencesCell Biologymedicine.diseaseMITOCHONDRIAL PERMEABILITY TRANSITIONApoptosisImmunologybiology.proteinNeuroscienceCell death and differentiation
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Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.

2014

Given our interest in finding potential antitumor agents and in view of the multifactorial mechanistic nature of cancer, in the present work, taking advantage of the multifunctional ligands approach, new chimeric molecules were designed and synthesized by combining in single chemical entities structural features of SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained by us and endowed with antiproliferative and pro-apoptotic activity. The new chimeric derivatives were characterized with respect to their cytotoxic activity and their effects on cell cycle progression on different tumor cell lines, as well as their HDACs inhibitio…

Multifunctional ligandsCell cycle progressionHDAC inhibitionInhibitory postsynaptic potentialBiochemistrySettore BIO/13 - Biologia ApplicataHDACDrug DiscoverymedicineCytotoxic T cellHDAC inhibition; Multifunctional ligands; antiproliferative activity; chimeric compound; stilbeneCancerbiologyChemistryANTIPROLIFERATIVE ACTIVITYOrganic ChemistryMultifunctional ligandsCancermultifunctional ligandmedicine.diseaseCombinatorial chemistrySettore CHIM/08 - Chimica FarmaceuticastilbeneHistoneBiochemistrySTILBENESbiology.proteinchimeric compoundHDAC INHIBITORSEpigeneticsHistone deacetylaseChimeric molecules
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