2021
Wet-dry-wet drug screen leads to the synthesis of TS1, a novel compound reversing lung fibrosis through inhibition of myofibroblast differentiation
Ring NAR, Volpe MC, Stepišnik T, Mamolo MG, Panov P, Kocev D, Vodret S, Fortuna S, Calabretti A, Rehman M, Colliva A, Marchesan P, Camparini L, Marcuzzo T, Bussani R, Scarabellotto S, Confalonieri M, Pham TX, Ligresti G, Caporarello N, Loffredo FS, Zampieri D, Džeroski S, Zacchigna S. Wet-dry-wet drug screen leads to the synthesis of TS1, a novel compound reversing lung fibrosis through inhibition of myofibroblast differentiation. Cell Death & Disease 2021, 13: 2. PMID: 34916483, PMCID: PMC8677786, DOI: 10.1038/s41419-021-04439-4.Peer-Reviewed Original ResearchConceptsAnti-fibrotic effectsDopamine receptor 3Lung fibrosisMyofibroblast activationReceptor 3Idiopathic pulmonary fibrosis patientsMyofibroblast differentiationPulmonary fibrosis patientsProgression of fibrosisTransforming Growth Factor-β PathwayGrowth factor β pathwayHigh-throughput screenDisease progressionMurine modelFibrosisFibrosis patientsFibrotic diseasesDrug screensLung fibroblastsNovel compoundsProgressionΒ pathwayImportant targetDopaminePrimary fibroblasts
2019
High-throughput screening discovers antifibrotic properties of haloperidol by hindering myofibroblast activation
Rehman M, Vodret S, Braga L, Guarnaccia C, Celsi F, Rossetti G, Martinelli V, Battini T, Long C, Vukusic K, Kocijan T, Collesi C, Ring N, Skoko N, Giacca M, Del Sal G, Confalonieri M, Raspa M, Marcello A, Myers MP, Crovella S, Carloni P, Zacchigna S. High-throughput screening discovers antifibrotic properties of haloperidol by hindering myofibroblast activation. JCI Insight 2019, 4: e123987. PMID: 30996132, PMCID: PMC6538355, DOI: 10.1172/jci.insight.123987.Peer-Reviewed Original ResearchMeSH KeywordsActinsAnimalsCalciumCell DifferentiationCells, CulturedDisease Models, AnimalDrug RepositioningEndoplasmic Reticulum StressFibrosisHaloperidolHumansIntravital MicroscopyLungMiceMyocardiumMyofibroblastsOptical ImagingPrimary Cell CultureReceptor, Notch1Receptors, sigmaRNA InterferenceRNA, Small InterferingSignal TransductionConceptsMyofibroblast activationSigma receptor 1Smooth muscle actinDifferent animal modelsTransforming Growth FactorDiscovery of haloperidolTumor-associated fibrosisMechanism of actionEndoplasmic reticulum stress responseFibrotic burdenAntifibrotic effectsAntifibrotic propertiesCommon antipsychotic drugsAntipsychotic drugsFibrotic processIntracellular calciumReticulum stress responseAnimal modelsMuscle actinFibrotic conditionsHaloperidolReceptor 1Growth factorContractile proteinsTherapeutic solutions
2018
Taming the Notch Transcriptional Regulator for Cancer Therapy
Tamagnone L, Zacchigna S, Rehman M. Taming the Notch Transcriptional Regulator for Cancer Therapy. Molecules 2018, 23: 431. PMID: 29462871, PMCID: PMC6017063, DOI: 10.3390/molecules23020431.Peer-Reviewed Original ResearchMeSH KeywordsCell DifferentiationCell ProliferationGene Expression Regulation, NeoplasticHumansNeoplasmsReceptors, NotchSignal TransductionSmall Molecule Libraries