Search results for "HCT116 cell"

showing 2 items of 52 documents

Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

2016

New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S ph…

antiproliferative activitybis-indolyl alkaloidsIndolesStereochemistryPopulationPharmaceutical ScienceAntineoplastic AgentsAntiproliferative activity; Apoptosis; Bis-indolyl alkaloids; Marine alkaloids; Thiazolyl-indolesBis-indolyl alkaloid010402 general chemistry01 natural sciencesArticlechemistry.chemical_compoundCell Line TumorDrug DiscoveryHumansCytotoxic T cellThiazolyl-indoleThiazoleMode of actioneducationlcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)Antitumor activityIndole testeducation.field_of_study010405 organic chemistryChemistryCell CycleImidazolesapoptosisApoptosiHCT116 CellsSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesThiazoleslcsh:Biology (General)BiochemistryApoptosisCell cultureMCF-7 Cellsmarine alkaloidsMarine alkaloidthiazolyl-indolesDrug Screening Assays Antitumormarine alkaloids; bis-indolyl alkaloids; thiazolyl-indoles; apoptosis; antiproliferative activityMarine Drugs
researchProduct

EGF-Induced Acetylation of Heterogeneous Nuclear Ribonucleoproteins Is Dependent on KRAS Mutational Status in Colorectal Cancer Cells.

2015

KRAS mutational status is considered a negative predictive marker of the response to anti-EGFR therapies in colorectal cancer (CRC) patients. However, conflicting data exist regarding the variable response to EGFR-targeted therapy. The effects of oncogenic KRAS on downstream targets were studied in cell lines with different KRAS mutations. Cells harboring a single KRASG13D allele showed the most tumorigenic profile, with constitutive activation of the downstream pathway, rendering them EGF-unresponsive. Conversely, KRASA146T cells showed a full EGF-response in terms of signal transduction pathways, cell proliferation, migration or adhesion. Moreover, the global acetylome of CRC cells was al…

lcsh:MedicineBiologymedicine.disease_causeHeterogeneous-Nuclear RibonucleoproteinsProto-Oncogene Proteins p21(ras)Epidermal growth factorCell Line TumormedicineHumansCell adhesionlcsh:ScienceMutationMultidisciplinaryEpidermal Growth FactorCell growthlcsh:RAcetylationCell migrationHCT116 CellsGene Expression Regulation NeoplasticDrug Resistance NeoplasmAcetylationMutationCancer researchlcsh:QKRASSignal transductionColorectal NeoplasmsResearch ArticleSignal TransductionPLoS ONE
researchProduct