Search results for "DISCOVERY"

showing 10 items of 4119 documents

From a Better Understanding of the Mechanisms of Action of Histone Deacetylases Inhibitors to the Progress of the Treatment of Malignant Lymphomas an…

2017

Background Notable progress has been made in chemo- and immunotherapy of B-cell lymphomas, but less in the treatment of T-cell lymphomas. Objective Histone deacetylases inhibitors are a potentially useful therapeutic mean, as an epigenetic dysregulation is present in lymphomas, and especially in T-cell types. We aimed to study the progress made in this area. Method A mini-review was achieved using the articles published in PubMed in the last two years and the new patents made in this field. Results Histone deacetylases inhibitors are involved in the derepression of tumor suppressor genes through a histone deacetylase-mediated transcriptional process. Their inhibition is followed by cell cyc…

Cancer ResearchDrug exportmedicine.medical_treatmentCellular differentiationAntineoplastic Agents010402 general chemistryLymphoma T-Cell01 natural sciencesHistone DeacetylasesRomidepsinPatents as TopicDrug DiscoveryPlasma Cell MyelomamedicineAnimalsHumansPharmacology (medical)Epigeneticsbiology010405 organic chemistrybusiness.industryDrug SynergismGeneral MedicineImmunotherapymedicine.diseasePeripheral T-cell lymphoma0104 chemical sciencesHistone Deacetylase InhibitorsHistoneOncologyDrug DesignImmunologyCancer researchbiology.proteinbusinessMultiple Myelomamedicine.drugRecent patents on anti-cancer drug discovery
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Synthetic Glycopeptides from the Mucin Family as Potential Tools in Cancer Immunotherapy

2006

Compared to glycoproteins of healthy cells, glycoproteins of tumor cells are often aberrantly glycosylated. Thus, glycopeptide fragments of surface glycoproteins of tumor cells are of interest as tumor-associated antigens for the distinction between normal and tumor cells. Cancer immunotherapy directed at selectively targeting these tumor-associated glycoprotein structure alterations--deficient glycosylation and, thus, exposure of peptide epitopes which are masked in normal cells--is considered a promising approach for the treatment of cancer. For this purpose, glycoproteins from the mucin family are of particular interest. Mucins belong to a class of heavily O-glycosylated, high-molecular …

Cancer ResearchGlycosylationmedicine.medical_treatmentAntineoplastic AgentsBiologyEpitopechemistry.chemical_compoundCancer immunotherapyAntigenNeoplasmsDrug DiscoverymedicineAnimalsHumansCytotoxic T cellPharmacologychemistry.chemical_classificationMucinGlycopeptidesMucinsImmunotherapy ActiveGlycopeptideOncologyBiochemistrychemistryMultigene FamilyGlycoproteinCurrent Cancer Drug Targets
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Development of resistance towards artesunate in MDA-MB-231 human breast cancer cells.

2011

Breast cancer is the most common cancer and the second leading cause of cancer death in industrialized countries. Systemic treatment of breast cancer is effective at the beginning of therapy. However, after a variable period of time, progression occurs due to therapy resistance. Artesunate, clinically used as anti-malarial agent, has recently revealed remarkable anti-tumor activity offering a role as novel candidate for cancer chemotherapy. We analyzed the anti-tumor effects of artesunate in metastasizing breast carcinoma in vitro and in vivo. Unlike as expected, artesunate induced resistance in highly metastatic human breast cancer cells MDA-MB-231. Likewise acquired resistance led to abol…

Cancer ResearchPhytochemistryPhytopharmacologyCancer TreatmentArtesunateApoptosisElectrophoretic Mobility Shift AssayDrug resistanceNude MiceMetastasischemistry.chemical_compoundMiceMolecular Cell BiologyDrug DiscoveryBreast TumorsBasic Cancer ResearchMedicinebcl-2-Associated X ProteinMultidisciplinaryQRNF-kappa BArtemisininsChemistryOncologyMedicineFemaleMatrix Metalloproteinase 1Breast carcinomamedicine.drugResearch Article570Drugs and DevicesDrug Research and DevelopmentCell SurvivalScienceMice Nude570 Life SciencesBreast NeoplasmsTumor Cell Line610 Medical Sciences MedicineBreast cancerComplementary and Alternative MedicineCell Line TumorAnimalsHumansDoxorubicinBiologyNeoplasm Drug Resistancebusiness.industryCancers and NeoplasmsChemotherapy and Drug Treatmentmedicine.diseaseXenograft Model Antitumor AssaysTranscription Factor AP-1chemistryTumor progressionArtesunateDrug Resistance NeoplasmCancer cellImmunologyEthnopharmacologyCancer researchbusinessPloS one
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Rad51 and BRCA2 - New Molecular Targets for Sensitizing Glioma Cells to Alkylating Anticancer Drugs

2011

First line chemotherapeutics for brain tumors (malignant gliomas) are alkylating agents such as temozolomide and nimustine. Despite growing knowledge of how these agents work, patients suffering from this malignancy still face a dismal prognosis. Alkylating agents target DNA, forming the killing lesion O(6)-alkylguanine, which is converted into DNA double-strand breaks (DSBs) that trigger apoptosis. Here we assessed whether inhibiting repair of DSBs by homologous recombination (HR) or non-homologous end joining (NHEJ) is a reasonable strategy for sensitizing glioma cells to alkylating agents. For down-regulation of HR in glioma cells, we used an interference RNA (iRNA) approach targeting Ra…

Cancer Treatmentlcsh:MedicineApoptosisToxicologyBiochemistrychemistry.chemical_compoundDrug DiscoveryRNA Small Interferinglcsh:ScienceHomologous RecombinationNeurological TumorsGene knockdownMultidisciplinaryBrain NeoplasmsGliomaFlow CytometryNon-homologous end joiningOncologyPARP inhibitorMedicinemedicine.drugResearch ArticleBiotechnologyDrugs and DevicesDrug Research and DevelopmentDNA damageMorpholinesToxic AgentsOlaparibGliomaCell Line TumormedicineHumansBiologyAntineoplastic Agents AlkylatingProtein Kinase InhibitorsBRCA2 ProteinTemozolomideBase SequenceNimustinelcsh:RCancers and NeoplasmsChemotherapy and Drug Treatmentmedicine.diseasechemistryMicroscopy FluorescenceChromonesCancer researchlcsh:QRad51 RecombinaseDNA DamagePLoS ONE
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Pharmacogenomics of Cameroonian traditional herbal medicine for cancer therapy

2011

Abstract Ethnopharmacological relevance A socio-economic burden associated with cancers is reported in Africa. Ethnopharmacological usages such as immune and skin disorders, inflammatory, and others chould be considered when selecting plants used to treat cancer, since these reflect disease states bearing relevance to cancer or a cancer symptoms. Materials and methods Documented compounds of Cameroonian medicinal plants were used as keywords in the National Cancer Institute (NCI) database to establish a library of cytotoxic compounds. Cellular and pharmacogenomic profiling was then performed for the 10 most cytotoxic natural products. By COMPARE and hierarchical cluster analyses, candidate …

Candidate geneMicroarrayCell SurvivalPharmacologyInhibitory Concentration 50chemistry.chemical_compoundCell Line TumorDrug DiscoveryAnimalsCluster AnalysisHumansMedicineCameroonRNA MessengerMedicinal plantsMedicine African TraditionalPharmacologyPlants MedicinalNatural productDose-Response Relationship DrugTraditional medicinebiologybusiness.industryGene Expression ProfilingPlumbaginbiology.organism_classificationAntineoplastic Agents PhytogenicGene Expression Regulation NeoplasticGene expression profilingchemistryDrug Resistance NeoplasmPharmacogeneticsPharmacogenomicsPlant PreparationsDiospyros crassiflorabusinessJournal of Ethnopharmacology
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Pharmacogenomics: a tool to prevent and cure coronary heart disease.

2007

Inflammation and genetics play an important role in the pathogenesis of coronary heart disease (CHD). This is supported by epidemiological studies which have thoroughly investigated the association between CHD and gene polymorphisms of the inflammatory molecules. Moreover, efforts to find elective therapy have not been rewarding and, despite the increasing appreciation of the role of genetics in CHD and myocardial infarction (MI) pathogenesis, pharmacogenomic approaches to uncover drug target have not been extensively explored. A critical search of published literature has suggested few inflammatory genes directly involved in the risk to develop CHD and MI. The selected genes are, the pro- …

Candidate genepharmacogenomicLipoxygenaseLipopolysaccharide ReceptorsMyocardial InfarctionCoronary DiseaseDiseaseBioinformaticsRisk AssessmentPathogenesisRisk FactorsDrug DiscoverymedicinecytokineHumansGenetic Predisposition to DiseaseMyocardial infarctionTLR4PharmacologyInflammationPolymorphism Geneticbusiness.industryPatient SelectionCase-control studyCOXLOXmedicine.diseaseAtherosclerosisToll-Like Receptor 4Treatment OutcomePharmacogeneticsProstaglandin-Endoperoxide SynthasesPharmacogenomicsCase-Control StudiesImmunologyCytokinesReceptors ChemokineChemokinesbusinessRisk assessmentCD14CCR5PharmacogeneticsCurrent pharmaceutical design
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Subsynaptic Distribution, Lipid Raft Targeting and G Protein-Dependent Signalling of the Type 1 Cannabinoid Receptor in Synaptosomes from the Mouse H…

2021

Numerous studies have investigated the roles of the type 1 cannabinoid receptor (CB1) in glutamatergic and GABAergic neurons. Here, we used the cell-type-specific CB1 rescue model in mice to gain insight into the organizational principles of plasma membrane targeting and Gαi/o protein signalling of the CB1 receptor at excitatory and inhibitory terminals of the frontal cortex and hippocampus. By applying biochemical fractionation techniques and Western blot analyses to synaptosomal membranes, we explored the subsynaptic distribution (pre-, post-, and extra-synaptic) and CB1 receptor compartmentalization into lipid and non-lipid raft plasma membrane microdomains and the signalling properties.…

Cannabinoid receptorG proteinhippocampusPharmaceutical ScienceHippocampusOrganic chemistryanti-CB1 antibodyGTP-Binding Protein alpha Subunits Gi-GoInhibitory postsynaptic potentialArticlerescue modelAnalytical ChemistryGlutamatergicMiceQD241-441Membrane MicrodomainsReceptor Cannabinoid CB1Drug Discoverytype 1 cannabinoid receptor CB1AnimalsPhysical and Theoretical ChemistryLipid raftMice KnockoutChemistryfrontal cortexmusculoskeletal neural and ocular physiologyfood and beveragescholesterolsynaptosomesEndocannabinoid systemCell biologyFrontal Lobenervous systemChemistry (miscellaneous)SynapsesMolecular MedicineGABAergiclipids (amino acids peptides and proteins)psychological phenomena and processesSignal TransductionMolecules (Basel, Switzerland)
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Increased endocannabinoid levels reduce the development of precancerous lesions in the mouse colon

2007

Colorectal cancer is an increasingly important cause of death in Western countries. Endocannabinoids inhibit colorectal carcinoma cell proliferation in vitro. In this paper, we investigated the involvement of endocannabinoids on the formation of aberrant crypt foci (ACF, earliest preneoplastic lesions) in the colon mouse in vivo. ACF were induced by azoxymethane (AOM); fatty acid amide hydrolase (FAAH) and cannabinoid receptor messenger ribonucleic acid (mRNA) levels were analyzed by the quantitative reverse transcription polymerase chain reaction (RT-PCR); endocannabinoid levels were measured by liquid chromatography-mass spectrometry; caspase-3 and caspase-9 expressions were measured by W…

Cannabinoid receptormedicine.medical_treatment2-Arachidonoylglycerolpreneoplastic lesionsMass Spectrometrychemistry.chemical_compoundMice0302 clinical medicineFatty acid amide hydrolaseDrug DiscoveryFatty acid amide hydrolase (FAAH)Aberrant crypt fociGenetics(clinical)ReceptorReceptors CannabinoidGenetics (clinical)Medicine(all)0303 health sciencesCaspase 3Reverse Transcriptase Polymerase Chain ReactionEndocannabinoid systemCaspase 93. Good health2-arachidonoylglycerolColon cancer030220 oncology & carcinogenesisColonic NeoplasmsMolecular Medicinelipids (amino acids peptides and proteins)psychological phenomena and processesRapid CommunicationAberrant crypt focimedicine.medical_specialtyColonAzoxymethaneBiologydigestive systemAmidohydrolases03 medical and health sciencesInternal medicineCannabinoid Receptor ModulatorsmedicineAnimalsRNA MessengerCannabinoid receptors030304 developmental biologyAzoxymethaneendocannabinoiddigestive system diseasesEndocrinologychemistrynervous systemCancer researchCannabinoidcancer pharmacologyPrecancerous ConditionsEndocannabinoids
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Zur Permeation der Serumeiwei�e in die Haut und ihrer quantitativen Bestimmung am Modell der Cantharidenblase

1964

Mittels chemischer und immunochemischer Methoden wurde vergleichend der Gehalt an Proteinen in Cantharidenblasen und Blutserum bestimmt. Erstmals werden auch quantitative Untersuchungen von Praalbumin, α2-M-Globulin, Coeruloplasmin, Haptoglobin und Transferrin im Cantharidenblaseninhalt vorgenommen. Dabei fanden sich statistisch gesicherte Unterschiede zwischen Cantharidenblasen- und Seruminhalt im Sinne tieferer Werte in den Blasen bei Gesamteiweis, Praalbumin abs., α2-M-Globulin abs., α2-Globulin abs. und rel.-%, Coeruloplasmin abs., β-Globulin abs., Transferrin abs. und γ-Globulin abs. Albumin abs. und rel.-% wiesen signifikante Unterschiede in Richtung hoherer Werte in den Cantharidenbl…

Cantharidinchemistry.chemical_compoundChemistryDrug DiscoveryMolecular MedicineCantharidesGeneral MedicineBlood proteinsMolecular biologyGenetics (clinical)Klinische Wochenschrift
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Quantitative Analysis of Terpenic Compounds in Microsamples of Resins by Capillary Liquid Chromatography

2019

A method has been developed for the separation and quantification of terpenic compounds typically used as markers in the chemical characterization of resins based on capillary liquid chromatography coupled to UV detection. The sample treatment, separation and detection conditions have been optimized in order to analyze compounds of different polarities and volatilities in a single chromatographic run. The monoterpene limonene and the triterpenes lupeol, lupenone, &beta

Capillary actionMonoterpenePharmaceutical Science01 natural sciencesArticlecapillary liquid chromatography (Cap-LC)Analytical Chemistrylcsh:QD241-441Terpenechemistry.chemical_compoundlcsh:Organic chemistryLimit of DetectiontriterpenesDrug DiscoveryTree resinPhysical and Theoretical ChemistryLupeolDetection limitLimoneneChromatographymicrosamplesMolecular Structure010405 organic chemistryTerpenes010401 analytical chemistryOrganic Chemistry0104 chemical scienceschemistryresinsChemistry (miscellaneous)Molecular MedicinelimoneneQuantitative analysis (chemistry)Resins PlantChromatography LiquidMolecules
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