A5044189374- Advanced biosensing and bioanalysis techniques
- DNA and Nucleic Acid Chemistry
- SARS-CoV-2 and COVID-19 Research
- Phosphodiesterase function and regulation
- RNA Interference and Gene Delivery
- Chemical Synthesis and Analysis
- Organoselenium and organotellurium chemistry
- Click Chemistry and Applications
- RNA and protein synthesis mechanisms
- Tryptophan and brain disorders
- Maternal Mental Health During Pregnancy and Postpartum
- Computational Drug Discovery Methods
- Synthesis and Characterization of Pyrroles
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Biological Activity
- Chemical synthesis and alkaloids
- Diverse Scientific Research Studies
- Psychedelics and Drug Studies
- Chemical Reaction Mechanisms
- Neurotransmitter Receptor Influence on Behavior
- Organic Chemistry Cycloaddition Reactions
- Cystic Fibrosis Research Advances
- Monoclonal and Polyclonal Antibodies Research
- Bacteriophages and microbial interactions
- Medicinal Plants and Neuroprotection
University of Brescia
2021-2024
University of Padua
2020
Istituto di Farmacologia Traslazionale
2020
In the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) genome, open reading frames (ORFs) encode for viral accessory proteins. Among these, Orf7a structurally resembles members of immunoglobulin (Ig) superfamily and intracellular adhesion molecules (ICAMs), in particular. ICAMs are involved integrin binding through lymphocyte function-associated antigen 1 (LFA-1). Based on such considerations previous findings SARS-CoV, it has been postulated that formation LFA-1/Orf7a complex...
While the neurochemistry that underpins behavioral phenotypes of depression is subject many studies, oxidative stress caused by inflammation comorbid with has not adequately been addressed. In this study, we described novel antidepressant-antioxidant agents consisting selenium-modified fluoxetine derivatives to simultaneously target serotonin reuptake (antidepressant action) and stress. Excitingly, show one these (
The spread of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) caused a worldwide outbreak coronavirus disease 19 (COVID-19), which rapidly evolved as global concern. efforts the scientific community are pointed towards identification promptly available therapeutic options. RNA-dependent RNA polymerase (RdRp) is promising target for developing small molecules to contrast SARS-CoV-2 replication. Modern computational tools can boost and repurposing known drugs targeting RdRp. We...
Fluoxetine finds application in the treatment of depression and mood disorders. This selective serotonin-reuptake inhibitor (SSRI) also contrasts oxidative stress by direct ROS scavenging, modulation endogenous antioxidant defense system, and/or enhancement serotonin capacity. We synthesised some fluoxetine analogues incorporating a selenium nucleus, thus expanding its potential enabling hydroperoxides-inactivating, glutathione peroxidase (GPx)-like activity. Radical scavenging peroxidatic...
In the central nervous system, some specific phosphodiesterase (PDE) isoforms modulate pathways involved in neuronal plasticity. Accumulating evidence suggests that PDE9 may be a promising therapeutic target for neurodegenerative diseases. current study, computational techniques were used to identify nature-inspired inhibitor bearing scaffold of an isoflavone, starting from database synthetic small molecules using ligand-based approach. Furthermore, docking studies supported by molecular...
We discuss a novel selenium-based reaction mechanism consisting in selenoxide elimination-triggered enamine hydrolysis. This one-pot model was studied for set of substrates. Under oxidative conditions, we observed and characterized the formation primary secondary amines as elimination products such compounds, paving way strategy to selectively release bioactive molecules. The underlying investigated using NMR, mass spectrometry density functional theory (DFT).
Guanine-rich sequences forming G-quadruplexes (GQs) are present in several genomes, ranging from viral to human. Given their peculiar localization, the induction of GQ formation or stabilization with small molecules represents a strategy for interfering crucial biological functions. Investigating recognition event at molecular level, aim fully understanding triggered pharmacological effects, is challenging. Native electrospray ionization mass spectrometry (ESI-MS) being optimized study these...
In drug discovery, ligand-mediated stabilization of G-quadruplexes is pursued for regulating gene expression and key cellular processes. Electrospray ionization mass spectrometry (ESI-MS) has been optimized screening putative DNA-binding small molecules natural synthetic origin. Several flavonoids were reported to interact with G-quadruplex, quercetin among them. this contribution, the interaction G-quadruplex DNA rutin, a glycoside extracted from flower buds Styphnolobium japonicum (L.)...
Isoflavones are listed among the most widely studied natural compounds in light of their several biological properties, one which consists ability to inhibit phosphodiesterases (PDEs).
The development of inhibitors that target the papain-like protease (PLpro) has potential to counteract spread severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), agent causing disease 2019 (COVID-19). Based on a consideration its several downstream effects, interfering with PLpro would both revert immune suppression exerted by virus and inhibit viral replication. By following repurposing strategy, current study evaluates antimalarial drugs as inhibitors, thereby possibility their...
Guanine-rich sequences of nucleic acids, including DNA and RNA, are known to fold into non-canonical structures named G-quadruplexes (G4s). Such arrangements these macromolecular polymers mainly located in telomeres promoter regions oncogenes and, for this reason, they represent a potential target compounds with therapeutic applications. In fact, the ligand-mediated stabilization G4s inhibits telomerase activity transcriptional machinery counteracts cancer cell immortalization. Flavonoids,...
G-quadruplex DNA is the target of several natural and synthetic small molecules with antiproliferative antiviral activity. We here report synthesis through Sonogashira reaction A3 coupling a disubstituted anthracene derivative, 9,10-bis[(4-(2-hydroxyethyl)piperazine-1-yl)prop-2-yne-1-yl]anthracene. The binding this compound to double stranded sequences was evaluated using electrospray ionization mass spectrometry (ESI-MS), demonstrating selectivity for first structure. interaction pattern...
4′-Methyl-4,5′-bithiazoles were previously identified as cystic fibrosis transmembrane regulator (CFTR) correctors, thus being able to correct folding defective mutants of the channel regulating chloride transport through membrane. Additionally, bithiazole derivative C17 was reported recover α-sarcoglycan in vitro and vivo. We report here synthesis two new derivatives C17, which sides scaffold modified. The synthesized compounds corresponding precursors tested myogenic cells evaluate...
Guanine-rich sequences are known to fold into G-quadruplex (G4) arrangements, which present in oncogenes and the telomeric regions of chromosomes. In particular, G4s represent an obstacle functioning telomerase, enzyme overexpressed cancer cells causing their immortalization. Therefore, G4 stabilization using small molecules represents appealing strategy for medicinal chemist. Ligands based on anthraquinone scaffold, peptidic side chains were attached by amide bond, previously reported. We...