A5003044125- Analytical Chemistry and Chromatography
- Molecular spectroscopy and chirality
- Protein Interaction Studies and Fluorescence Analysis
- Drug Transport and Resistance Mechanisms
- Asymmetric Synthesis and Catalysis
- Computational Drug Discovery Methods
- Analytical Methods in Pharmaceuticals
- Antibiotics Pharmacokinetics and Efficacy
- Spectroscopy and Quantum Chemical Studies
- Neuroscience and Neuropharmacology Research
- Mass Spectrometry Techniques and Applications
- Monoclonal and Polyclonal Antibodies Research
- Chromatography in Natural Products
- Synthesis of β-Lactam Compounds
- Inorganic and Organometallic Chemistry
- Cancer Treatment and Pharmacology
- Microfluidic and Capillary Electrophoresis Applications
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Chemical synthesis and alkaloids
- Various Chemistry Research Topics
- Glycosylation and Glycoproteins Research
- Photoreceptor and optogenetics research
- Axial and Atropisomeric Chirality Synthesis
- Cholinesterase and Neurodegenerative Diseases
University of Bologna
2013-2023
Centre Hospitalier Universitaire de Tours
2013
National Research Council
2011
Institute of Organic Synthesis and Photoreactivity
2004-2011
Indena (Italy)
2003-2008
University of Ferrara
2007
University of Florence
1995-2007
Uppsala University
2005
Saarland University
2005
University of Basilicata
2005
Abstract The initial transition of amyloid β (1–42) (Aβ42) soluble monomers/small oligomers from unordered/α‐helix to a β‐sheet‐rich conformation represents suitable target design new potent inhibitors and obtain effective therapeutics for Alzheimer's disease. Under optimized conditions, this reliable reproducible CD kinetic study showed three‐step sigmoid profile that was characterized by lag phase (prevailing conformation), an exponential growth (increasing β‐sheet secondary structure)...
In this study, the systemic assessments of stereoisomers triazole fungicide difenoconazole are reported for first time, including absolute stereochemistry, stereoselective bioactivity toward pathogens (Alternaria sonali, Fulvia fulva, Botrytis cinerea, and Rhizoctonia solani), toxicity aquatic organisms (Scenedesmus obliquus, Daphnia magna, Danio rerio). Moreover, degradation in vegetables (cucumber, Cucumis sativus tomato, Lycopersicon esculentum) under field conditions soil...
Beside the regulation of fluid distribution, human serum albumin (HSA) carries other activities, such as binding, transport, and detoxification many molecules. In patients with cirrhosis, HSA exhibits posttranscriptional alterations that likely affect its functions. This study aimed at identifying structural occurring in cirrhosis determining their relationship specific clinical complications patient survival. One hundred sixty-eight 35 stable conditions 133 hospitalized for acute...
We reported previously that Bcl-2 is paradoxically down-regulated in paclitaxel-resistant cancer cells. reveal here paclitaxel directly targets the loop domain, thereby facilitating initiation of apoptosis. Molecular modeling revealed an extraordinary similarity between binding sites and beta-tubulin, leading us to speculate could be mimetic endogenous peptide ligand, which binds both proteins. tested hypothesis mimics Nur77, which, like paclitaxel, changes function Bcl-2. This premise was...
SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as member of RNA polymerase complex, and its oncogenic has been described different cancer types. We studied the expression activity preclinical model colorectal (CRC) found it strongly upregulated throughout tumorigenesis both at mRNA protein level. Our results also showed RNAi‐mediated ablation impairs CRC cell proliferation indicating required for proper growth. These data, together with...
Combined results of theoretical molecular dynamic simulations and in vitro spectroscopic (circular dichroism fluorescence) studies are presented, providing the atomistic secondary structure details process by which a selected small molecule may destabilize β-sheet ordered "amyloid" oligomers formed model undecapeptide amyloid β-peptide 25-35 [Aβ(25-35)]. Aβ(25-35) was chosen because it is shortest fragment capable forming large fibrils retaining toxicity full length Aβ(1-40/42) peptides. The...
We report the discovery of compound 4a, a potent β-lactam-based monoacylglycerol lipase (MGL) inhibitor characterized by an irreversible and stereoselective mechanism action, high membrane permeability, brain penetration evaluated using human in vitro blood-brain barrier model, selectivity binding affinity-based proteomic profiling assays, low toxicity. Mode-of-action studies demonstrate that blocking MGL, increases 2-arachidonoylglycerol behaves as cannabinoid (CB1/CB2) receptor indirect...
Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed our immunohistochemistry studies on HDAC6 overexpression in tissues. We herein developed series of novel hHDAC6 inhibitors, having low inhibitory potency over hHDAC1 and hHDAC8, as potential pharmacological tools for treatment. Their was combined vitro vivo toxicity. Structural analysis 6h structure–activity...
Abstract A human serum albumin‐based HPLC chiral stationary phase (HSA‐CSP) has been examined as a tool to investigate binding of drugs HSA and drug–drug protein‐binding interactions. Rac‐oxazepam hemisuccinate (OXH) was used model compound the chromatographic retention ( k ′) its enantiomers determined after addition displacers mobile phase. Compounds known bind at same site OXH different sites were tested for their displacing capacities. Competitive interactions between in reflected by...
Abstract Drug binding to albumins from different mammalian species was investigated disclose evidence of species‐dependent stereoselectivity in drug‐binding processes and affinities. This aspect is important for evaluating the reliability extrapolating distribution data among species. The circular dichroism (CD) signal induced by drug [human serum albumin (HSA), bovine (BSA), rat (RSA), dog (DSA)] were measured analyzed. selected drugs metabolites HSA significantly differed other terms...
Decompensated cirrhosis is associated to extensive post-transcriptional changes of human albumin (HA). This study aims characterize the occurrence HA homodimerization in a large cohort patients with decompensated and evaluate its association clinical features prognosis. monomeric dimeric isoforms were identified peripheral blood by using HPLC-ESI-MS technique 123 cirrhotic hospitalized for acute decompensation 50 age- sex-comparable healthy controls. Clinical biochemical parameters recorded...
The water-soluble complex derived from Rh(CO)2(acac) and human serum albumin (HSA) proved to be efficient in the hydroformylation of several olefin substrates. chemoselectivity regioselectivity were generally higher than those obtained by using classic catalytic systems like TPPTS-Rh(I) (TPPTS=triphenylphosphine-3,3′,3″-trisulfonic acid trisodium salt). Styrene 1-octene, for instance, converted almost quantitative yields into corresponding oxo-aldehydes at 60 °C 70 atm (CO/H2=1) even very...
Abstract A circular dichroism‐based detection system presents several advantages in the HPLC analysis of chiral compounds because selective monitoring optically active molecules. Its use allows reliable determination enantiomeric excesses and elution order. To this end, application empirical, semiempirical, nonempirical methods to get stereochemical information from CD signal is reported. Furthermore, recording spectra on line evaluation dissymetry factor make very powerful characterizing...