Search results for "topoi"

showing 10 items of 701 documents

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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Synergistic cytotoxic interactions between sodium butyrate, MG132 and camptothecin in human retinoblastoma Y79 cells.

2000

This paper studies the effects caused in human retinoblastoma Y79 cells by treatment with combinations of sodium butyrate, the inhibitor of topoisomerase I camptothecin and the inhibitor of 26S proteasome MG132. The combination of sodium butyrate and camptothecin resulted in a strong synergistic cytotoxicity, as revealed by combination indices of 0.77 and 0.52 calculated at IC(50) and IC(75). Synergistic interactions were also demonstrated for combinations of sodium butyrate and MG132, camptothecin and MG132 and for a combination of all three compounds. The cytotoxic effects observed after the combined treatments can be considered a consequence of apoptosis, as suggested by the appearance o…

medicine.drug_classCell SurvivalLeupeptinsSodiumchemistry.chemical_elementApoptosisButyrateBiologyCysteine Proteinase Inhibitorschemistry.chemical_compoundMG132Antineoplastic Combined Chemotherapy ProtocolsmedicineTumor Cells CulturedHumansheterocyclic compoundsEnzyme InhibitorsRetinoblastomaCaspase 3TopoisomeraseRetinoblastomaSodium butyrateDrug SynergismGeneral Medicinemedicine.diseaseeye diseasesEnzyme ActivationButyrateschemistryBiochemistryProto-Oncogene Proteins c-bcl-2CaspasesCancer researchbiology.proteinCamptothecinTopoisomerase I InhibitorsTumor Suppressor Protein p53CamptothecinTopoisomerase inhibitormedicine.drugTumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine
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Repurposing of the ALK inhibitor crizotinib for acute leukemia and multiple myeloma cells

2021

Crizotinib was a first generation of ALK tyrosine kinase inhibitor approved for the treatment of ALK-positive non-small-cell lung carcinoma (NSCLC) patients. COMPARE and cluster analyses of transcriptomic data of the NCI cell line panel indicated that genes with different cellular functions regulated the sensitivity or resistance of cancer cells to crizotinib. Transcription factor binding motif analyses in gene promoters divulged two transcription factors possibly regulating the expression of these genes, i.e., RXRA and GATA1, which are important for leukemia and erythroid development, respectively. COMPARE analyses also implied that cell lines of various cancer types displayed varying degr…

medicine.drug_classPharmaceutical Scienceacute myeloid leukemiaArticletranscriptomicsPharmacy and materia medicaDrug Discoverytyrosine kinase inhibitorsmedicineCytotoxic T cellnetwork pharmacologyddc:610biologyCrizotinibdrug repurposingChemistryTopoisomeraseRMyeloid leukemiaCell cyclemedicine.diseaseALK inhibitorRS1-441multiple myelomaLeukemiaCancer cellbiology.proteinCancer researchMolecular MedicineMedicinemedicine.drug
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Design, synthesis, DNA-binding and cytotoxicity evaluation of new potential combilexines

2002

Combilexines, compounds in which a DNA intercalator is linked to a minor groove binding component, interact with the DNA in a sequence specific manner to yield in most cases compounds with anticancer activity. A series of new compounds closely related to netropsin in which the two components were linked by an amide group was synthesised as potential combilexines. As some of these compounds showed cytotoxic activity in vitro, an attempt was made to rationalise their mechanism of action. The DNA binding characteristics of the carboxamides were evaluated by thermal denaturation experiments and by ethidium bromide displacement assay. Their ability to inhibit the topoisomerase I was also determi…

medicine.drug_classStereochemistryAntineoplastic AgentsCarboxamideNucleic Acid DenaturationChemical synthesischemistry.chemical_compoundDrug DiscoveryTumor Cells CulturedmedicineA-DNAPharmacologyBinding SitesbiologyTopoisomeraseOrganic ChemistryDNAGeneral MedicineIntercalating AgentschemistryMechanism of actionBiochemistryNetropsinDrug Designbiology.proteinDrug Screening Assays AntitumorTopoisomerase I Inhibitorsmedicine.symptomEthidium bromideCell DivisionDNAEuropean Journal of Medicinal Chemistry
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Impact of Prophylactic CD8-Depleted Donor-Lymphocyte Infusions After Allogeneic Hematopoietic Stem Cell Transplantation and Alemtuzumab Mediated T-Ce…

2011

Abstract Abstract 4109 We have previously demonstrated that the application of CD8-depleted donor-lymphocyte infusions (DLI) is feasible after reduced-intensity conditioning and in vivo T-cell depletion by alemtuzumab. DLI overcome slow lymphocyte recovery associated with alemtuzumab-administration and improve anti-infectious immunity and reliably convert a decreasing T-cell chimerism (Meyer et al. Blood 2007 & BMT 2010). Here we provide clinical follow up data of 117 patients with different hematological diseases and a median observation time of 1 year (range, 1–86 months) post hematopoietic stem cell transplantation (HSCT). The majority of patients either suffered from an acute leukem…

medicine.medical_specialtyAcute leukemiabusiness.industrymedicine.medical_treatmentImmunologyContext (language use)Cell BiologyHematologyHematopoietic stem cell transplantationmedicine.diseaseBiochemistryGastroenterologySurgeryTransplantationGraft-versus-host diseaseInternal medicinemedicineAlemtuzumabbusinessSurvival analysisMultiple myelomamedicine.drugBlood
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Toxoplasmosis after hematopoietic stem transplantation. Report of a 5-year survey from the Infectious Diseases Working Party of the European Group fo…

2000

Toxoplasmosis after hematopoietic stem transplantation. Report of a 5-year survey from the Infectious Diseases Working Party of the European Group for Blood and Marrow Transplantation

medicine.medical_specialtyBone marrow transplantPremedicationAntibodies ProtozoanBlood DonorsOpportunistic InfectionsImmunocompromised HostSeroepidemiologic StudiesInternal medicineTrimethoprim Sulfamethoxazole Drug CombinationEpidemiologymedicineAnimalsHumansTransplantation HomologousTransplantationMarrow transplantationbusiness.industryHematopoietic Stem Cell TransplantationHematologymedicine.diseaseToxoplasmosisTransplantationHaematopoiesissurgical procedures operativeImmunologybusinessToxoplasmaDisease transmissionToxoplasmosisBone Marrow Transplantation
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Cationic lipide mediated transfer of c-abl and bcr antisense oligonucleotides to immature normal myeloid cells: Uptake, biological effects and modula…

1996

Uptake and biochemical and biological effects of antisense oligodeoxynucleotides (ODN) specific for c-abl and bcr genes were studied in normal immature myeloid cells. CD34-positive cells were purified by positive and negative selection and cultured in liquid culture for 7 days. These cells were then incubated with ODNs, either alone or in combination with cationic lipids. The uptake of ODNs was enhanced by the use of cationic lipids. In addition, very low concentrations of ODNs in combination with cationic lipids were capable of specifically inhibiting the expression of the c-abl gene. In contrast, no effects were seen on the expression of bcr. However, despite the effective blocking of c-a…

medicine.medical_specialtyCell Membrane PermeabilityChemical PhenomenaMolecular Sequence DataRibonuclease HAntigens CD34BiologyTransfectionPolymerase Chain ReactionCationsProto-Oncogene Proteinshemic and lymphatic diseasesInternal medicineGene expressionmedicineHumansCation Exchange ResinsRNA NeoplasmProto-Oncogene Proteins c-ablGeneCells CulturedOncogene ProteinsABLHematologyBase SequenceCell-Free SystemChemistry PhysicalCell growthCationic polymerizationbreakpoint cluster regionBiological Transporthemic and immune systemsHematologyGeneral MedicineOligonucleotides AntisenseProtein-Tyrosine Kinasesrespiratory systemHematopoietic Stem CellsLipidsMolecular biologyHaematopoiesisGene Expression RegulationDepression ChemicalLiposomesProto-Oncogene Proteins c-bcrAnnals of Hematology
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A single high dose of idarubicin combined with high-dose ARA-C for treatment of first relapse in childhood ‘high-risk’ acute lymphoblastic leukaemia:…

2002

The outcome of children with acute lymphoblastic leukaemia (ALL) and early relapse remains unsatisfactory. In January 1995, the AIEOP (Associazione Italiana di Oncologia ed Ematologia Pediatrica) group opened a trial for children with ALL in first isolated or combined bone marrow relapse defined at high risk according to the length of first remission and the immunophenotype. The treatment plan included the combination of a single high-dose idarubicin and high-dose cytarabine as induction therapy followed by an intensive consolidation and stem cell transplant (SCT). In total, 100 children from 16 Italian centres were enrolled; 80 out of the 99 evaluable patients (81%) achieved second complet…

medicine.medical_specialtyChemotherapybusiness.industrymedicine.drug_classmedicine.medical_treatmentHematologyHematopoietic stem cell transplantationmedicine.diseaseAntimetaboliteSurgerymedicine.anatomical_structureInternal medicineAcute lymphocytic leukemiaCytarabineMedicineIdarubicinBone marrowbusinessSurvival ratemedicine.drugBritish Journal of Haematology
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Guidelines for the management of cytomegalovirus infection in patients with haematological malignancies and after stem cell transplantation from the …

2018

Summary Cytomegalovirus is one of the most important infections to occur after allogeneic haematopoietic stem cell transplantation (HSCT), and an increasing number of reports indicate that cytomegalovirus is also a potentially important pathogen in patients treated with recently introduced drugs for hematological malignancies. Expert recommendations have been produced by the 2017 European Conference on Infections in Leukaemia (ECIL 7) after a review of the literature on the diagnosis and management of cytomegalovirus in patients after HSCT and in patients receiving other types of therapy for haematological malignancies. These recommendations cover diagnosis, preventive strategies such as pr…

medicine.medical_specialtyCongenital cytomegalovirus infectionCytomegalovirusAntiviral AgentsLetermovirInternal medicinemedicineHumansIn patientGanciclovirLeukemiabusiness.industryHematopoietic Stem Cell TransplantationMaribavirmedicine.diseaseTransplantationClinical trialHaematopoiesisInfectious DiseasesHematologic NeoplasmsCytomegalovirus InfectionsPractice Guidelines as TopicBenzimidazolesRibonucleosidesStem cellbusinessmedicine.drugThe Lancet. Infectious diseases
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Consensus on performing skin biopsies, laboratory workup, evaluation of tissue samples and reporting of the results in patients with suspected cutane…

2014

Background Histopathological diagnosis including selection of lesions, the determination of the best point of time for biopsy and workup is not trivial in cutaneous graft-versus-host disease (GvHD). Objectives To develop interdisciplinary recommendations on performing, the laboratory work up and reporting of the results of skin biopsies in patients with suspected cutaneous GvHD. Methods A working group consisting of dermatopathologists, dermatologists, transplant-physicians and transplant-pathologists prepared recommendations for performing skin biopsies, laboratory workup and evaluation of tissue samples, and reporting of the results in patients with cutaneous GvHD. After achieving a conse…

medicine.medical_specialtyConsensusBiopsymedicine.medical_treatmentMedizinGraft vs Host DiseaseDermatologyDiseaseSkin Diseasesimmune system diseasesSurveys and QuestionnairesBiopsyHumansTransplantation HomologousMedicineIn patientSkinintegumentary systemmedicine.diagnostic_testbusiness.industryHistological TechniquesHematopoietic Stem Cell TransplantationImmunosuppressionCutaneous graft-versus-host diseaseDermatologyWork-upSurgeryTransplantationsurgical procedures operativeInfectious DiseasesAcute DiseaseChronic DiseaseSkin biopsybusiness
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