Search results for "proteinas"

showing 10 items of 416 documents

Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates

2018

A family of dipeptidyl enoates has been prepared and tested against the parasitic cysteine proteases rhodesain, cruzain and falcipain-2 related to sleeping sickness, Chagas disease and malaria, respectively. They have also been tested against human cathepsins B and L1 for selectivity. Dipeptidyl enoates resulted to be irreversible inhibitors of these enzymes. Some of the members of the family are very potent inhibitors of parasitic cysteine proteases displaying k2nd (M−1s−1) values of seven orders of magnitude. In vivo antiprotozoal testing was also performed. Inhibitors exhibited IC50 values in the micromolar range against Plasmodium falciparum, Trypanosoma brucei, Trypanosoma cruzi and ev…

0301 basic medicinesleeping sicknessClinical BiochemistryPharmaceutical Science01 natural sciencesBiochemistryCathepsin BinhibitorsDrug Discoverychemistry.chemical_classificationbiologyChemistryDipeptidesHep G2 CellsMolecular Docking SimulationCysteine EndopeptidasesBiochemistryAntiprotozoalMolecular MedicineChagas diseaseProteasesCell Survivalmedicine.drug_classPlasmodium falciparumTrypanosoma brucei bruceimalariaAntiprotozoal AgentsCysteine Proteinase InhibitorsTrypanosoma bruceicysteine proteasesInhibitory Concentration 50Structure-Activity Relationship03 medical and health sciencesparasitic diseasesmedicineHumansTrypanosoma cruziMolecular Biologychagas diseaseBinding Sites010405 organic chemistryOrganic ChemistryPlasmodium falciparumbiology.organism_classificationmedicine.diseaseProtein Structure Tertiary0104 chemical sciences030104 developmental biologyEnzymeCysteineBioorganic & Medicinal Chemistry
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Genotyping strategy of SMAD-3 rs3825977 gene variant for a differential management of ascending aorta aneurysm in women people: Gender oriented diagn…

2020

Abstract Background and objectives The research of opportune strategies for facilitating the management of complex pathologies, such as ascending aorta aneurysm (AAA), currently represents the principal object of clinicians, clinical pathologists included. Herein, we propose genotyping of gene variants related to TGF-β pathway as useful strategy to improve the complex AAA management, exclusively based on imaging evaluations. Precisely, we investigated four functional SNPs in SMAD and VEGF genes, encoding molecules able to modulate functions and cross-talks of TGF-β pathway. Populations and methods Our study included 92 individuals (70 men (76%) and 22 (24%) women; mean age: 71.4 ± 2.6 years…

0301 basic medicinetransforming growth factorSNPs of SMAD and VEGF genesSMADBioinformaticsAscending aorta aneurysm (AAA)03 medical and health sciences0302 clinical medicineImmune systemmedicine.arteryGenotypeGeneticsmedicineGenotypingGeneGenetics (clinical)aorta aneurysmMetalloproteinaseAortaFemale peoplebusiness.industryGenetic variantsaorta aneurysm; transforming growth factorSettore MED/23030104 developmental biology030220 oncology & carcinogenesisGender medicinebusinessGenotyping strategy
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Functional characterization of Coat Protein I (COPI) subunit isoforms in Arabidopsis thaliana

2022

La vía secretora temprana implica el transporte bidireccional entre el retículo endoplásmico (ER) y el aparato de Golgi y está mediada por vesículas recubiertas del complejo de proteína de cubierta I (COPI) y del complejo de proteína de cubierta II (COPII). Las vesículas COPII están involucradas en el transporte del RE al aparato de Golgi, mientras que las vesículas COPI median el transporte intra-Golgi y el transporte retrógrado desde el aparato de Golgi al RE. El componente clave de la cubierta de COPI es un complejo citoplasmático denominado coatómero, que se compone de siete subunidades (α/β/β’/γ/δ/ε/ζ) y se recluta en bloque desde el citosol hacia las membranas de Golgi. Se ha descrito…

:CIENCIAS DE LA VIDA::Biología celular [UNESCO]vía secretoracoatomerovesiculas copitráfico de proteinasUNESCO::CIENCIAS DE LA VIDA::Biología celularisoformas
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Determinantes estructurales del plegamiento y la interacción entre fragmentos transmembrana

2003

El análisis de secuencias genómicas completas de diversos organismos muestra que, aproximádamente, un 20-30% de las pautas de lectura abierta codifica para proteínas que atraviesan la membrana (Arkin, Brunger et al. 1997) (Wallin and von Heijne 1998). Sin embargo el medio en que estas proteínas adoptan su estructura nativa y desarrollan su función, la membrana, ha dificultado la aplicación directa de las técnicas de estudio habituales para proteínas solubles. Esta dificultad se refleja en el hecho de que en la era de la explosción de obtención de estructuras proteícas de alta resolución, se limita a unas docenas el número de proteínas de membrana resueltas. En este trabajo se…

:CIENCIAS DE LA VIDA::Bioquímica [UNESCO]UNESCO::CIENCIAS DE LA VIDA::Biología molecularbioquímicaUNESCO::CIENCIAS DE LA VIDA::Bioquímicaglicoforina A (GpA)proteinas:CIENCIAS DE LA VIDA::Biología molecular [UNESCO]
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Effect of a dominant-negative form of ADAM10 in a mouse model of Alzheimer's disease.

2009

The alpha-secretase cleaves in the non-amyloidogenic pathway the amyloid-beta protein precursor (AbetaPP) within the region of the amyloid-beta peptides to prevent their formation and aggregation in the brain. Members of the ADAM family (a disintegrin and metalloprotease) are the main candidates for physiologically relevant alpha-secretases. We recently demonstrated that overexpression of ADAM10 in mice transgenic for human AbetaPP (ADAM10 x APP[V717I]) alleviated functional deficits related to Alzheimer's disease. To further demonstrate that this is due to the specific activity of alpha-secretase, we characterized mice overexpressing an inactive form of ADAM10 (ADAM10[E384A]; ADAM10-dn). T…

ADAM10Morris water navigation taskGlutamic AcidStimulationMice TransgenicADAM10 ProteinAmyloid beta-Protein PrecursorMiceIn vivoAlzheimer DiseaseDisintegrinReaction TimeAnimalsHumansIsoleucineProtein precursorMaze LearningSwimmingMetalloproteinaseAlaninebiologyBehavior AnimalChemistryGeneral NeuroscienceAge FactorsMembrane ProteinsValineGeneral MedicineCell biologyMice Inbred C57BLPsychiatry and Mental healthClinical PsychologyADAM ProteinsDisease Models Animalbiology.proteinSpecific activityGeriatrics and GerontologyAmyloid Precursor Protein SecretasesJournal of Alzheimer's disease : JAD
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MMP-2, MMP-9 and activin A blood levels in patients with breast cancer or prostate cancer metastatic to the bone.

2007

Background: The clinical significance of the circulating levels of activin A and matrix metalloproteinase-2 (MMP-2) and -9 (MMP-9) was investigated in patients with breast cancer (BC) or prostate cancer (PC) with (M1) or without (M0) bone metastasis. Patients and Methods: MMP-2, MMP-9 and activin A blood concentrations were measured by enzyme immunoassays in 79 cancer patients and in 57 healthy blood donors (HS) who served as a control group. The diagnostic accuracy of these molecules to discriminate between M0 and M1 patients was evaluated by the receiver operating characteristic curve (ROC) and compared to that of tumor markers CA15.3 or prostate-specific antigen (PSA). Results: Activin A…

AdultAged 80 and overMaleMucin-1Prostatic NeoplasmsBone NeoplasmsBreast NeoplasmsMiddle AgedActivinsActivin Breast Cancer Bone metastasis proteinasesMatrix Metalloproteinase 9Activins; Adult; Aged; Aged 80 and over; Bone Neoplasms; Breast Neoplasms; Female; Humans; Male; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Middle Aged; Mucin-1; Prostatic NeoplasmsHumansMatrix Metalloproteinase 2FemaleAged
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MMP-7 promoter polymorphisms do not influence CD4+ recovery and changes in plasma viral load during antiretroviral therapy for HIV-1 infection.

2005

Summary Matrix metalloproteinase-7 (MMP-7) generates soluble Fas Ligand (FasL), which is involved in the apoptotic loss of CD4+ T cells during HIV infection. We evaluated whether two polymorphisms in MMP-7 promoter could influence CD4+ recover in response to antiretroviral therapy, and found that these polymorphisms are ineffective.

AdultCD4-Positive T-LymphocytesMaleImmunologyHuman immunodeficiency virus (HIV)HIV InfectionsMatrix metalloproteinasemedicine.disease_causeMMP-7; Fas ligand; CD4T cells; HIV infectionFas ligandPlasma viral loadGeneticsHumansMedicineMolecular BiologyGenetics (clinical)Polymorphism Geneticbusiness.industryMetalloendopeptidasesGeneral MedicineMiddle AgedViral LoadAntiretroviral therapySoluble fas ligandCD4 Lymphocyte CountAnti-Retroviral AgentsApoptosisMatrix Metalloproteinase 7ImmunologyHIV-1business
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Expression of adhesion factors and degrading proteins in primary and secondary glioblastomas and their precursor tumors.

2000

In tumor tissue specimens of 27 primary and 17 secondary glioblastomas and the precursor lesions, the immunohistochemical expression patterns of the membrane protein CD44s, the basal lamina proteins laminin, collagen IV, and fibronectin, the lectin galectin-3 recognizing tenascin and N-CAM as well as of the matrix-degrading enzymes matrix metalloproteinase MMP-2 and MMP-9, and cathepsin D were studied. Besides expression of basal lamina proteins in vessels, all glioblastomas and the precursor lesions showed strong immunoreactivity of CD44s, tenascin, galectin-3, and N-CAM which were restricted to solid tumor masses. Present in solid tumor areas, MMP-2, MMP-9 and cathepsin D were also strong…

AdultCancer Researchanimal structuresGalectin 3TenascinCathepsin DBiologyAstrocytomaCathepsin DLamininGliomamedicineHumansCell adhesionNeural Cell Adhesion MoleculesBrain NeoplasmsMiddle Agedmedicine.diseaseMolecular biologyAntigens DifferentiationImmunohistochemistryMatrix MetalloproteinasesFibronectinsFibronectinmedicine.anatomical_structureHyaluronan ReceptorsMembrane proteinMatrix Metalloproteinase 9biology.proteinMatrix Metalloproteinase 2Basal laminaCollagenLamininNeoplasm Recurrence LocalGlioblastomaInvasionmetastasis
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Zymographic analysis of circulating and tissue forms of colon carcinoma gelatinase A (MMP-2) and B (MMP-9) separated by mono- and two-dimensional ele…

2001

Gelatinase A (MMP-2) and gelatinase B (MMP-9) play a key role in the proteolytic cascade leading to ECM degradation during invasion and metastasis. The enzyme activity is regulated both at the intra- and extra-cellular level. Extracellular regulation is achieved mainly through the balance between proenzyme activation and inhibition, which appears to be altered in cancer patients. One of the mechanisms of MMP inhibition is the binding of the enzymes to appropriate tissue inhibitors (TIMP). In the recent literature, it has been suggested that MMP-2 and/or MMP-9 are indeed over-produced in many carcinomas, while the identity of the various enzymatic forms (latent, activated and enzyme/inhibito…

AdultGelatin ZymographyGelatinase AMatrix metalloproteinaseBiologyMetastasisExtracellularmedicineGelatinaseHumansElectrophoresis Gel Two-DimensionalMolecular Biologychemistry.chemical_classificationEnzyme Precursorsmedicine.diseaseMolecular biologyEnzyme assayEnzymeBiochemistrychemistryMatrix Metalloproteinase 9Colonic Neoplasmsbiology.proteinMatrix Metalloproteinase 2Electrophoresis Polyacrylamide GelDensitometryMatrix biology : journal of the International Society for Matrix Biology
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Enzymatic modification of low-density lipoprotein in the arterial wall: a new role for plasmin and matrix metalloproteinases in atherogenesis.

2004

Objective— Functionally interactive proteases of the plasminogen/plasmin and the matrix metalloproteinase (MMP) system degrade and reorganize the extracellular matrix of the vessel wall in atherosclerosis. Here we investigated whether such proteases are able to confer atherogenic properties onto low density lipoprotein by nonoxidative modification. Methods and Results— Similar to the recently described enzymatically-modified low-density lipoprotein (E-LDL), native LDL exposed to plasmin or matrix MMP-2 or MMP-9 and cholesterylester-hydrolase (CEH) showed extensive deesterification, with ratios of free cholesterol to total cholesterol rising to 0.8 compared with 0.2 in native LDL. When the …

AdultLipoprotein modificationProteasesAdolescentPlasminArteriosclerosisBlotting WesternMatrix metalloproteinaseComplement Hemolytic Activity AssayMonocyteschemistry.chemical_compoundmedicineHumansTrypsinFibrinolysinComplement ActivationCells CulturedAgedbiologyMacrophagesAntibodies MonoclonalSodium Dodecyl SulfateLipoprotein(a)Middle AgedSterol EsteraseCell biologyLipoproteins LDLC-Reactive ProteinchemistryBiochemistryMatrix Metalloproteinase 9Low-density lipoproteinbiology.proteinMatrix Metalloproteinase 2lipids (amino acids peptides and proteins)Electrophoresis Polyacrylamide GelCardiology and Cardiovascular MedicinePlasminogen activatormedicine.drugLipoproteinArteriosclerosis, thrombosis, and vascular biology
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