Search Results - "COSTANTINO, Gabriele"
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New promises for manipulation of kynurenine pathway in cancer and neurological diseases
Published in Expert opinion on therapeutic targets (01-02-2009)“…The kynurenine pathway (KP), the primary route of tryptophan degradation in mammalian cells, consists of a cascade of enzymatic reactions eventually leading to…”
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2
Extraction and Quantification of Azelaic Acid from Different Wheat Samples ( Triticum durum Desf. ) and Evaluation of Their Antimicrobial and Antioxidant Activities
Published in Molecules (Basel, Switzerland) (24-02-2023)“…Azelaic Acid (AzA) is a 9-carbon atom dicarboxylic acid, with numerous pharmacological uses in dermatology. Its effectiveness in papulopustular rosacea and…”
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Integration of Enhanced Sampling Methods with Saturation Transfer Difference Experiments to Identify Protein Druggable Pockets
Published in Journal of chemical information and modeling (26-03-2018)“…Saturation transfer difference (STD) is an NMR technique conventionally applied in drug discovery to identify ligand moieties relevant for binding to protein…”
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Amine- and Amino Acid-Based Compounds as Carbonic Anhydrase Activators
Published in Molecules (Basel, Switzerland) (02-12-2021)“…After being rather neglected as a research field in the past, carbonic anhydrase activators (CAAs) were undoubtedly demonstrated to be useful in diverse…”
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Inhibition studies of bacterial α-carbonic anhydrases with phenols
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2022)“…The α-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogens (NgCAα) and (VchCAα) were investigated for their inhibition by a panel of…”
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Development of Praziquantel sulphonamide derivatives as antischistosomal drugs
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2022)“…The almost empty armamentarium to treat schistosomiasis, a neglected parasitic disorder caused by trematode flatworms of the genus Schistosoma, except…”
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Alpha-synuclein/synapsin III pathological interplay boosts the motor response to methylphenidate
Published in Neurobiology of disease (01-05-2020)“…Loss of dopaminergic nigrostriatal neurons and fibrillary α-synuclein (α-syn) aggregation in Lewy bodies (LB) characterize Parkinson's disease (PD). We…”
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Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases
Published in Journal of medicinal chemistry (25-06-2015)“…This study describes the discovery of novel dengue virus inhibitors targeting both a crucial viral protein–protein interaction and an essential host cell…”
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Inhibitors of the sulfur assimilation pathway in bacterial pathogens as enhancers of antibiotic therapy
Published in Current medicinal chemistry (01-01-2015)“…The rising emergence of antibiotic resistance urges the search for new strategies to defeat microorganisms that lead to persistent infections of the host…”
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Preliminary structure−activity relationships analysis on N-(3,5-dichlorophenyl)-4,5-dihydronaphtho[1,2-d]thiazol-2-amine, a disruptor of mycobacterial energetics
Published in Medicinal chemistry research (01-03-2024)“…The increasing emergence of drug-resistance among mycobacteria represents a serious global health threat, requiring novel and effective therapeutic strategies…”
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LiGen: A High Performance Workflow for Chemistry Driven de Novo Design
Published in Journal of chemical information and modeling (24-06-2013)“…Tools for molecular de novo design are actively sought incorporating sets of chemical rules for fast and efficient identification of structurally new…”
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Farnesoid X Receptor: From Structure to Potential Clinical Applications
Published in Journal of medicinal chemistry (25-08-2005)Get full text
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13
Evaluation of oxidative stress markers in Rwanda during the SARS-CoV-2 pandemic: A cross-sectional study
Published in PLOS global public health (25-10-2023)“…COVID-19 is mainly described as endothelial dysfunction, and due to the bidirectional link between oxidative stress and endothelial dysfunction, we initiated a…”
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14
Pharmacophore modeling and virtual screening studies to identify novel selective SIRT2 inhibitors
Published in Journal of molecular graphics & modelling (01-06-2019)“…Sirtuins (SIRTs) are a class of NAD+-dependent protein histone deacetylases (HDACs) that catalyse the reversible deacetylation of lysine residues in the…”
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Chemical Markers in Italian Propolis: Chrysin, Galangin and CAPE as Indicators of Geographic Origin
Published in Plants (Basel) (01-10-2024)“…Knowledge of the chemical composition of propolis is crucial for understanding the characteristics of products of different origins, but also for quality…”
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Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief
Published in Proceedings of the National Academy of Sciences - PNAS (25-11-2014)“…Significance Persistent pain in inflammatory and neuropathic conditions is often refractory to conventional analgesic therapy, with most patients suffering…”
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Inhibition of O-acetylserine sulfhydrylase by fluoroalanine derivatives
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…O-acetylserine sulfhydrylase (OASS) is the pyridoxal 5′-phosphate dependent enzyme that catalyses the formation of L-cysteine in bacteria and plants. Its…”
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The Aryl Hydrocarbon Receptor (AhR) Mediates the Counter-Regulatory Effects of Pelargonidins in Models of Inflammation and Metabolic Dysfunctions
Published in Nutrients (07-08-2019)“…Pelargonidins are anthocyanidins thought to be beneficial for the human health, although controversies exist over the doses needed and the unclear mechanism of…”
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Porous titanium microsphere kyphoplasty for augmentation treatment of osteoporotic vertebral fractures: Technical report and case series
Published in Frontiers in surgery (03-05-2023)“…Vertebral augmentation procedures (VAPs) are used in cases of persistent and unresponsive pain in patients with vertebral compression fractures (VCFs)…”
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Irreversible Inhibition of Epidermal Growth Factor Receptor Activity by 3-Aminopropanamides
Published in Journal of medicinal chemistry (08-03-2012)“…Irreversible epidermal growth factor receptor (EGFR) inhibitors contain a reactive warhead which covalently interacts with a conserved cysteine residue in the…”
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