Search Results - "Fiorito, Jole"
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Synaptic Therapy in Alzheimer’s Disease: A CREB-centric Approach
Published in Neurotherapeutics (2015)“…Therapeutic attempts to cure Alzheimer’s disease (AD) have failed, and new strategies are desperately needed. Motivated by this reality, many laboratories…”
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Synaptic and memory dysfunction induced by tau oligomers is rescued by up-regulation of the nitric oxide cascade
Published in Molecular neurodegeneration (27-06-2019)“…Soluble aggregates of oligomeric forms of tau protein (oTau) have been associated with impairment of synaptic plasticity and memory in Alzheimer's disease…”
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Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells
Published in Journal of medicinal chemistry (10-11-2016)“…(±)-MRJF22 [(±)-2], a novel prodrug of haloperidol metabolite II (sigma-1 receptor antagonist/sigma-2 receptor agonist ligand) obtained by conjugation to…”
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Correction: Synaptic and memory dysfunction induced by tau oligomers is rescued by up-regulation of the nitric oxide cascade
Published in Molecular neurodegeneration (29-04-2024)Get full text
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Development of novel phosphodiesterase 5 inhibitors for the therapy of Alzheimer’s disease
Published in Biochemical pharmacology (01-06-2020)“…[Display omitted] Nitric oxide (NO) is a gaseous molecule that plays a multifactorial role in several cellular processes. In the central nervous system, the NO…”
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Identification of a Novel 1,2,3,4-Tetrahydrobenzo[b][1,6]naphthyridine Analogue as a Potent Phosphodiesterase 5 Inhibitor with Improved Aqueous Solubility for the Treatment of Alzheimer’s Disease
Published in Journal of medicinal chemistry (09-11-2017)“…Phosphodiesterase 5 (PDE5) hydrolyzes cyclic guanosine monophosphate (cGMP) leading to increased levels of the cAMP response element binding protein (CREB), a…”
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Optimizing metabolic stability of phosphodiesterase 5 inhibitors: Discovery of a potent N-(pyridin-3-ylmethyl)quinoline derivative targeting synaptic plasticity
Published in Bioorganic & medicinal chemistry letters (15-08-2023)“…[Display omitted] Phosphodiesterase 5 (PDE5) is a cyclic guanosine monophosphate-degrading enzyme involved in numerous biological pathways. Inhibitors of PDE5…”
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Histone Acetyltransferase (HAT) Activator, YF2, Modulates the p53:BCL6 Axis and Antigen Presentation in Diffuse Large B-Cell Lymphomas
Published in Blood (23-11-2021)“…A hallmark of DLBCL is epigenetic derangements characterized by monoallelic mutations in histone acetyltransferases (HATs); EP300 (p300) and CREBBP (CBP). The…”
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PDE5 Exists in Human Neurons and is a Viable Therapeutic Target for Neurologic Disease
Published in Journal of Alzheimer's disease (26-04-2016)“…Phosphodiesterase 5 (PDE5) is a critical component of the cGMP-PKG axis of cellular signaling in neurons, and inhibition of PDE5 has been shown to be…”
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PDE5 inhibitors against synaptic and cognitive impairment in Alzheimer’s disease and related dementia
Published in Alzheimer's & dementia (01-12-2022)“…Background Gene transcription mechanisms leading to synaptic plasticity and memory formation, including phosphorylation of the transcription factor CREB, are…”
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Synthesis of quinoline derivatives: Discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease
Published in European journal of medicinal chemistry (01-02-2013)“…Phosphodiesterase type 5 (PDE5) mediates the degradation of cGMP in a variety of tissues including brain. Recent studies have demonstrated the importance of…”
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Strategy for Overcoming Crebbp and EP300 Mutations in Lymphoma: Development of First-in-Class HAT Activators
Published in Blood (13-11-2019)“…Epigenetic dysregulation is a hallmark of germinal center derived B cell lymphomas. In particular, the monoallelic mutations in histone acetyltransferases…”
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Haloperidol metabolite II prodrug: Asymmetric synthesis and biological evaluation on rat C6 glioma cells
Published in European journal of medicinal chemistry (27-01-2015)“…In a previous work we reported the antiproliferative effects of (±)-MRJF4, a novel haloperidol metabolite II (HP-mII) (a sigma-1 antagonist and sigma-2…”
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Development of First-in-Class Histone Acetyltransferase (HAT) Activators for Precision Targeting of Epigenetic Derangements in Lymphoma
Published in Blood (29-11-2018)“…Monoalleleic inactivating mutations in histone acetyltransferase (HAT) enzymes promote lymphomagenesis in germinal center derived B-cell lymphomas, follicular…”
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Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells
Published in European journal of medicinal chemistry (01-01-2011)“…Complex mechanisms of prostate cancer progression prompt to novel therapeutic strategies concerning a combination of drugs or of single molecules able to…”
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Effect of MRJF4 on C6 Glioma Cells Proliferation and Migration
Published in Central nervous system agents in medicinal chemistry (2017)“…MRJF4, a novel haloperidol metabolite II prodrug, was obtained through the esterification of the secondary hydroxyl group of haloperidol metabolite II with…”
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