Giuseppe D’Orazio

ORCID: 0000-0003-4101-2908
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About
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Research Areas
  • Carbohydrate Chemistry and Synthesis
  • Glycosylation and Glycoproteins Research
  • Chemical Synthesis and Analysis
  • Synthetic Organic Chemistry Methods
  • Microbial Metabolites in Food Biotechnology
  • Bioactive Compounds and Antitumor Agents
  • Probiotics and Fermented Foods
  • Alzheimer's disease research and treatments
  • Microbial Natural Products and Biosynthesis
  • Supramolecular Self-Assembly in Materials
  • Click Chemistry and Applications
  • Cyclization and Aryne Chemistry
  • Biochemical and Molecular Research
  • Monoclonal and Polyclonal Antibodies Research
  • Gut microbiota and health
  • Chemical Synthesis and Reactions
  • Cholinesterase and Neurodegenerative Diseases
  • Amyloidosis: Diagnosis, Treatment, Outcomes
  • Cancer therapeutics and mechanisms
  • Nanocluster Synthesis and Applications
  • Immune cells in cancer
  • Polysaccharides and Plant Cell Walls
  • Ubiquitin and proteasome pathways
  • Medicinal Plants and Neuroprotection
  • Process Optimization and Integration

University of Milan
2010-2025

Polytechnic University of Bari
2024

University of Milano-Bicocca
2010-2020

Mylan (Switzerland)
2017

National Interuniversity Consortium of Materials Science and Technology
2013

Abstract Macrophages are crucial drivers of innate immunity. Reprogramming macrophages to a restorative phenotype in cancer or autoimmune diseases can stop their cancer‐promoting activity trigger anti‐inflammatory Glycans have emerged as key components for immunity they involved many pathophysiological disorders. Previous studies demonstrated that supraphysiological amounts mannose (Man) sialic acid (Sia) inhibit tumor growth and stimulate differentiation regulatory T cells. Man is known...

10.1002/advs.202407458 article EN cc-by Advanced Science 2025-02-14

Abstract Cancer aberrant N - and O -linked protein glycosylation, frequently resulting from an augmented flux through the Hexosamine Biosynthetic Pathway (HBP), play different roles in tumor progression. However, low specificity toxicity of existing HBP inhibitors prevented their use for cancer treatment. Here we report preclinical evaluation FR054, a novel inhibitor enzyme PGM3, with remarkable anti-breast effect. In fact, FR054 induces breast cells dramatic decrease cell proliferation...

10.1038/s41419-018-0405-4 article EN cc-by Cell Death and Disease 2018-03-07

Sodium–glucose co-transporter 1 (SGLT1) and sodium-dependent neutral amino acid transporter (B0AT1) are mainly expressed on the membrane of enterocytes, a type epithelial cell found in intestines. In addition to their physiological role absorption nutrients, protective integrity intestinal barrier has been established. The natural ligands SGLT1 (d-glucose) B0AT1 (l-glutamine) can trigger anti-inflammatory effect epithelium. literature suggests activation common intracellular pathways upon...

10.3390/app14062248 article EN cc-by Applied Sciences 2024-03-07

Over the last decades, a novel immunological function was established for sodium–glucose co-transporter 1 (SGLT1), protein involved in sugar absorption small intestine. High-glucose dosage and pharmacological concentrations of C-glucoside analog showed protective role vitro vivo models severe inflammation states; experimental evidence suggests engagement SGLT1 these processes. The mechanism action underlying protection is still unclear. To enhance our understanding molecular mechanisms...

10.3390/m1982 article EN cc-by Molbank 2025-03-21

Gold nanoparticles (AuNPs) are a promising tool for drug delivery due to their unique chemical properties that make them biocompatible and easy functionalize. However, when AuNPs introduced into biological systems, they coated by the so-called protein corona (PC), which affects biodistribution limits therapeutic efficacy. The functionalization of with endogenous carbohydrates can be possible strategy reduce immune recognition, thus enhancing biocompatibility circulation time. Suitable...

10.3390/m1985 article EN cc-by Molbank 2025-03-27

Sodium–glucose co-transporter 1 (SGLT1) is primarily expressed on the membrane of enterocytes, a type epithelial cell found in intestines, where it mediates unidirectional absorption glucose and galactose. Beyond its well-established role nutrient absorption, SGLT1 also plays protective maintaining integrity intestinal barrier. Specifically, natural ligand (d-glucose) synthetic C-glucoside developed by our group can induce anti-inflammatory effect epithelium. In this paper, we report...

10.3390/molecules29215067 article EN cc-by Molecules 2024-10-26

Background. Several research findings suggest that sodium–glucose co-transporter 1 (SGLT1) is implicated in the progression and control of infections inflammation processes at pulmonary level. Moreover, our previous works indicate an engagement SGLT1 inhibiting inflammatory response induced intestinal epithelial cells by TLR agonists. In this study, we report anti-inflammatory effects observed lung upon transporter, use glucose BLF501, a synthetic ligand, for treatment animal models...

10.3390/immuno4040031 article EN cc-by Immuno 2024-11-08

A small library of glycofused tricyclic compounds with a central pyran ring chemically modified in the position para to oxygen has been synthesised. The influence chemical modification on structural conformation and their ability bind Aβ peptide evaluated respectively using molecular mechanics (MM) dynamics (MD) simulations, STD NMR spectroscopy. introduction particularly polar/charged groups leads loss binding ability, without significant change conformation, whilst other substitutions does...

10.1002/asia.201501114 article EN Chemistry - An Asian Journal 2015-11-02

The use of cellulose nanocrystals (CNCs) as a biomaterial able to inhibit host cell bacterial adhesion is described. Pre-incubation of<italic>E. coli</italic>with suspension CNCs affords significant reduction intestinal monolayer HT29, without exerting bactericidal effect.

10.1039/c7tb01923h article EN Journal of Materials Chemistry B 2017-01-01

Abstract Background Recent studies demonstrated that engagement of sodium glucose transporter 1 (SGLT-1) by orally administered D-glucose protects the intestinal mucosa from lipopolysaccharide (LPS)-induced injury. We tested whether SGLT-1 might protect doxorubicin (DXR)- and 5-fluorouracil (5-FU)-induced injury in animal models mimicking acute or chronic mucositis. Methods Mice were treated intraperitoneally with DXR, alone combination 5-FU, BLF501, a glucose-derived synthetic compound high...

10.1186/1476-4598-13-23 article EN cc-by Molecular Cancer 2014-02-05

Abstract We synthesized fused bicyclic polyfunctional compounds containing a highly hydroxylated pyran ring starting from commercially available methyl glucopyranoside and adopting RCM annulation approach. The versatile α,β‐unsaturated ketone group was introduced on the newly formed and, as an example of potential these polyfunctionalized building blocks, tetracyclic compound through Diels–Alder cycloaddition reaction.

10.1002/ejoc.201400028 article EN European Journal of Organic Chemistry 2014-02-19

A new versatile thiophene derivative exomethylene-3,4-ethylenedioxythiophene (emEDOT) is introduced. The molecule can be straightforwardly prepared in two steps from commercially available derivatives and enables facile further derivatization through both acid catalyzed additions of alcohols standard thiol–ene click chemistry. preparation electrochromic materials an electrochemical avidine sensor shown by the oxidative polymerizations several functionalized EDOT monomers emEDOT.

10.1021/ol401008s article EN Organic Letters 2013-06-24

A library of GlcNAc 6‐ or 1‐phosphate analogues was designed, and each compound evaluated computationally through docking studies for its binding affinity to AGM1/PGM3. The compounds with the highest affinity, as ranked a score, were synthesised screened their ability inhibit production UDP‐GlcNAc. glycofused oxazoline analogue showed good inhibition, gave significant results in vitro.

10.1002/ejoc.201800183 article EN European Journal of Organic Chemistry 2018-03-15

Abstract The intricate nature of carbohydrate structures has prompted the scientific community to seek efficient protocols for their manipulation. Lengthy synthetic pathways, often necessary achieve complex sugar structures, pose challenges not only in terms time and cost but also regarding environmental sustainability. Consequently, domino transformations serve as valuable tools streamlining drug discovery processes. Sequential procedures involving fewer steps minimal isolation/purification...

10.1002/ejoc.202400511 article EN cc-by European Journal of Organic Chemistry 2024-08-10

Abstract We synthesized a small library of N‐ spirofused bicyclic derivatives 1‐deoxynojirimycin (DNJ), as quaternary ammonium salts, through double S N 2 annulation process. The rings are different size and structural characteristics. Preliminary biological evaluation showed no antibacterial activity towards both Gram+ Gram‐ bacteria. DNJ derivative bearing 6 member cycle revealed promising inhibitor amyloglucosidase. Binding energies calculated docking studies resembled the in vitro...

10.1002/slct.201600516 article EN ChemistrySelect 2016-07-01

A set of heterobifunctional oligo ethylene glycols have been synthesized in a straightforward and stepwise manner starting from inexpensive, commercially available, tetraethylene glycol. Introduction terminal allyl moieties followed by reductive ozonolysis allowed controlled elongation. Mono-allyl derivatives were used for the elongation with functionalized moiety successive introduction different functional groups on chain terminal.

10.1055/s-0032-1318433 article EN Synlett 2013-03-04

Abstract Fluorescent glycofused tricyclic compounds were synthesized through the domino conjugate oxa‐Michael addition/aldol condensation of 2‐hydroxybenzaldehydes with protected 3‐oxoglucal by exploiting activation an organocatalyst. Stereoselectivity was obtained using ( R )‐(+)‐α,α‐diphenyl‐2‐pyrrolidinemethanol trimethylsilyl ether as catalyst. All presented good optical properties. able to bind synthetic amyloid β 1–42 peptide aggregates and label plaques from brain sections transgenic...

10.1002/ejoc.201501593 article EN European Journal of Organic Chemistry 2016-03-01

Abstract C ‐Glucoside derivatives covalently linked to the arsenic atom in different oxidation states have been synthesized by avoiding protection‐deprotection steps. While compound 1 , bearing an As V atom, did not show any significant biological activity, 2 which glucose moiety is as dithioarsenical (As III ), showed promising antiproliferative activity on a cell line of neuroblastoma (SK‐N‐BE).

10.1002/ejoc.201500529 article EN European Journal of Organic Chemistry 2015-06-22
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