A5053103943- Immune Response and Inflammation
- Carbohydrate Chemistry and Synthesis
- Glycosylation and Glycoproteins Research
- Chemical Synthesis and Analysis
- Antimicrobial Peptides and Activities
- Remote Sensing and LiDAR Applications
- Protein Kinase Regulation and GTPase Signaling
- Influenza Virus Research Studies
- Pneumonia and Respiratory Infections
- Pediatric health and respiratory diseases
- Immune Cell Function and Interaction
- PI3K/AKT/mTOR signaling in cancer
- Remote Sensing in Agriculture
- Computational Drug Discovery Methods
- Heart Failure Treatment and Management
- Monoclonal and Polyclonal Antibodies Research
- Marine and coastal ecosystems
- Neonatal Respiratory Health Research
- Enzyme Production and Characterization
- Lipid Membrane Structure and Behavior
- Cardiac electrophysiology and arrhythmias
- Biochemical and Molecular Research
- Inflammatory mediators and NSAID effects
- Receptor Mechanisms and Signaling
- Ion channel regulation and function
University of Milano-Bicocca
2016-2025
University of Massachusetts Boston
2009-2019
Google (United States)
2018
Boston University
2009-2017
Mylan (Switzerland)
2016
University of Milan
2000-2014
University of Iowa
2011
University of Lausanne
1998-1999
Institute of Chemistry of Molecular Recognition
1999
University of Parma
1995-1998
Neuropathic pain remains a prevalent clinical problem because it is often poorly responsive to the currently used analgesics, thus crucial identification of new potential targets and drugs. Recent evidence indicated that microglial cells in spinal cord are critically involved development maintenance neuropathic pain, with pivotal role toll-like receptor 4 (TLR4). Binding an endogenous ligand TLR4 might be considered important step regulation microglia activity facilitation, suggesting...
Toll-like receptor 4 (TLR4), together with MD-2, binds bacterial endotoxins (E) high affinity, triggering formation of the activated homodimer (E.MD-2.TLR4)2. Activated TLR4 induces intracellular signaling leading to activation transcription factors that result in cytokine and chemokine production initiation inflammatory immune responses. also responds endogenous ligands called danger associated molecular patterns (DAMPs). Increased sensitivity infection a variety pathologies have been...
4-anilino quinazolines have been identified as inhibitors of HCV replication. The target this class compounds was proposed to be the viral protein NS5A, although unequivocal proof has never presented. A quinazoline moiety is often found in kinase inhibitors, leading us formulate hypothesis that anti-HCV activity displayed by these might due inhibition a cellular kinase. Type III phosphatidylinositol 4-kinase α (PI4KIIIα) recently host factor for We therefore evaluated AL-9, compound...
Abstract Dysregulated Toll-like receptor (TLR)-4 activation is involved in acute systemic sepsis, chronic inflammatory diseases, such as atherosclerosis and diabetes, viral infections, influenza infection. Thus, therapeutic control of the TLR4 signalling pathway major interest. Here we tested activity small-molecule synthetic antagonist, FP7, vitro on human monocytes monocyte-derived dendritic cells (DCs) vivo during virus infection mice. Our results indicate that FP7 antagonized secretion...
Abstract Modeling human neuronal properties in physiological and pathological conditions is essential to identify novel potential drugs explore mechanisms of neurological diseases. For this purpose, we generated a three-dimensional (3D) culture, by employing the readily available neuroblastoma SH-SY5Y cell line, new differentiation protocol. The entire process occurred matrix lasted 47 days, with 7 days pre-differentiation phase 40 differentiation, allowed development 3D culture consistent...
Cell metabolism now appears as an essential regulator of immune cells activation. In particular, TLR stimulation triggers metabolic reprogramming dendritic (DCs) with increased glycolytic flux, whereas inhibition glycolysis alters their functional The molecular mechanisms involved in the control upon are poorly understood for human DCs. TLR4 activation monocyte-derived DCs (MoDCs) stimulated glucose consumption and lactate production. Global hexokinase (HK) activity, controlling initial...
A thiophene-based donor-acceptor phenothiazine dye has been functionalized with a peripheral glucose unit (PTZ-GLU) to bust its affinity water and enhance dye-sensitized photogeneration of hydrogen. Compared the corresponding alkyl derivative (PTZ-ALK), as well common hydrophilic triethylene glycol substitution (PTZ-TEG), sugar shows lower contact angle; PTZ-GLU performed twice more efficient than PTZ-TEG in hydrogen terms evolved gas turnover number.
The structure–activity relationship was investigated in a series of synthetic TLR4 antagonists formed by glucosamine core linked to two phosphate esters and linear carbon chains. Molecular modeling showed that the compounds with 10, 12, 14 carbons chains are associated higher stabilization MD-2/TLR4 antagonist conformation than case C16 variant. Binding experiments human MD-2 C12 C14 variants have affinity C10, while variant did not interact protein. molecules, exception variant, inhibited...
Dye-sensitized photocatalytic H2 generation has been investigated using a metal-free phenothiazine-based donor–acceptor sensitizer (PTZ-GLU) in combination with coadsorbents. The coadsorption of the PTZ-GLU dye, functionalized glucose end-group, glucose-based coadsorbent, afforded improved activity compared to absence coadsorbents, use conventional (chenodeoxycholic acid) or by replacing dye functionality an alkyl chain. results suggest strategic role directional intermolecular...
We disclose here a panel of small-molecule TLR4 agonists (the FP20 series) whose structure is derived from previously developed ligands (FP18 series). The new molecules have increased chemical stability and shorter, more efficient, scalable synthesis. series showed selective activity as with potency similar to FP18. Interestingly, despite the similarity FP18 series, different mechanism action immunofluorescence microscopy no NF-κB nor p-IRF-3 nuclear translocation but rather MAPK...
New glycolipids and a benzylammonium lipid were rationally designed by varying the chemical structure of D-glucose-derived hit compound active as A antagonist. We report synthesis these compounds, their in vitro activity antagonists on HEK cells, capacity to inhibit LPS-induced septic shock vivo. The lack toxicity good vivo suggest use some compounds panel hits for antisepsis drug development.