0000000000141189

AUTHOR

Pier Giorgio Petronini

showing 4 related works from this author

Irreversible Inhibition of Epidermal Growth Factor Receptor Activity by 3-Aminopropanamides

2012

Irreversible epidermal growth factor receptor (EGFR) inhibitors contain a reactive warhead which covalently interacts with a conserved cysteine residue in the kinase domain. The acrylamide fragment, a commonly employed warhead, effectively alkylates Cys797 of EGFR, but its reactivity can cause rapid metabolic deactivation or nonspecific reactions with off-targets. We describe here a new series of irreversible inhibitors containing a 3-aminopropanamide linked in position 6 to 4-anilinoquinazoline or 4-anilinoquinoline-3- carbonitrile driving portions. Some of these compounds proved to be as efficient as their acrylamide analogues in inhibiting EGFR-TK (TK = tyrosine kinase) autophosphorylati…

AmideCell SurvivalEGFR inhibitorsQuinolineAntineoplastic AgentsAntineoplastic AgentStructure-Activity RelationshipT790MGefitinibCell Line TumorDrug DiscoveryPropionatemedicineHumansStructure–activity relationshipEpidermal growth factor receptorPhosphorylationAniline CompoundsbiologyChemistryDrug Discovery3003 Pharmaceutical ScienceAutophosphorylationQuinazolineAniline CompoundAmidesSettore CHIM/08 - Chimica FarmaceuticaErbB ReceptorsBiochemistryProtein kinase domainDrug Resistance NeoplasmQuinazolinesQuinolinesbiology.proteinMolecular MedicinePhosphorylationReceptor Epidermal Growth FactorPropionatesDrug Screening Assays AntitumorTyrosine kinaseHumanmedicine.drugJournal of Medicinal Chemistry
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Hypertonic Stress and Amino Acid Deprivation Both Increase Expression of mRNA for Amino Acid Transport System A

2004

The activity of amino acid transport system A ([Oxender and Christensen, 1963][1]) is regulated in a variety of different ways, the best studied being the increases of its activity caused by starving cells of amino acids or by exposing them to hypertonicity (for review see [McGivan and Pastor-

Amino Acid Transport System APhysiologyCHO CellsBiologyCricetulusOsmotic PressureCricetinaeAnimalsHumansOsmotic pressureRNA MessengerAmino AcidsLetter to the Editorchemistry.chemical_classificationRegulation of gene expressionMessenger RNAChinese hamster ovary cellbiology.organism_classificationAmino acidGene Expression RegulationHypotonic SolutionschemistryBiochemistryHypertonic StressTonicityCricetulusJournal of General Physiology
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Tumor-infiltrating lymphocytes and breast cancer: Beyond the prognostic and predictive utility

2017

The importance of the immune system as a potent anti-tumor defense has been consolidated in recent times, and novel immune-related therapies are today demonstrating a strong clinical benefit in the setting of several solid neoplasms. Tumor-infiltrating lymphocytes reflect the attempt of the host to eradicate malignancies, and during the last decades, they have been shown to possess an interesting prognostic utility for breast cancer, especially in case of HER2 positive and triple-negative molecular subtypes. In parallel, the clinical evaluation of tumor-infiltrating lymphocytes has been shown to effectively predict treatment outcomes in both neoadjuvant and adjuvant settings. Currently, tu…

Tumor-infiltrating lymphocytes; breast cancer; cancer immunotherapy0301 basic medicineOncologyCA15-3medicine.medical_specialtymedicine.medical_treatmentCA 15-3Tumor-infiltrating lymphocyteBreast NeoplasmsTumor-infiltrating lymphocytes03 medical and health sciencesLymphocytes Tumor-Infiltratingbreast cancer0302 clinical medicineImmune systemBreast cancerCancer immunotherapyInternal medicinemedicineHumansRC254-282cancer immunotherapyTumor-infiltrating lymphocytesbusiness.industryNeoplasms. Tumors. Oncology. Including cancer and carcinogensCancerGeneral MedicinePrognosismedicine.diseaseNeoadjuvant TherapyTreatment Outcome030104 developmental biologyImmunoediting030220 oncology & carcinogenesisFemalebusinessTumor Biology
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Stabilization of hsp70 mRNA on prolonged cell exposure to hypertonicity

2002

AbstractProlonged exposure of 3T3 cells to 0.5 osM hypertonic medium induced the accumulation of hsp70 mRNAs. This increase in mRNA levels required active protein synthesis. A weak and transient activation of heat shock factor 1 (HSF1) was noted, but it was temporally uncoupled to the accumulation of the hsp70 mRNAs. Nuclear run-on assay and transfection experiments showed that hsp70 gene transcription was not affected by hypertonicity. ActD chase experiments showed that during hypertonic treatment, degradation of hsp70 mRNAs was markedly reduced. This effect did not appear to be a general phenomenon since the increase in mRNA level of another gene induced by hypertonicity (ATA2 transporter…

Amino Acid Transport System ATranscription GeneticBiologyTransfectionMiceHeat Shock Transcription FactorsTranscription (biology)Heat shock proteinATA2 mRNAAnimalsHSP70 Heat-Shock ProteinsRNA MessengerHSF1HypertonicityMolecular BiologySaline Solution HypertonicMessenger RNAHeat shock proteinMRNA stabilizationTransfection3T3 CellsCell Biologyhsp70 mRNAMolecular biologyHsp70DNA-Binding ProteinsProtein BiosynthesisRNA stabilizationmRNA stabilizationTranscription FactorsBiochimica et Biophysica Acta (BBA) - Molecular Cell Research
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