A5060832175- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Biological Evaluation
- Protein Structure and Dynamics
- Calcium signaling and nucleotide metabolism
- ATP Synthase and ATPases Research
- Bioactive Compounds and Antitumor Agents
- Receptor Mechanisms and Signaling
- Synthesis of Organic Compounds
- Neuropeptides and Animal Physiology
- Enzyme Structure and Function
- RNA modifications and cancer
- Hemoglobin structure and function
- Insect Pest Control Strategies
- Reproductive Biology and Fertility
- Natural Compound Pharmacology Studies
- Glycosylation and Glycoproteins Research
- Nicotinic Acetylcholine Receptors Study
- Drug Transport and Resistance Mechanisms
- Metabolism and Genetic Disorders
- Metal-Catalyzed Oxygenation Mechanisms
- Carbohydrate Chemistry and Synthesis
- Metal complexes synthesis and properties
- Computational Drug Discovery Methods
Elettra-Sincrotrone Trieste S.C.p.A.
2023
Sapienza University of Rome
1994-2022
National Research Council
2021-2022
University of Trieste
2022
Institute of Molecular Biology and Pathology
2021-2022
Istituto Pasteur
2021
University of Rome Tor Vergata
2017
Abstract Dysregulation of calcium signaling is emerging as a key feature in the pathogenesis neurodegenerative diseases such Alzheimer’s disease (AD), Parkinson’s (PD), and Huntington’s (HD), targeting this process may be therapeutically beneficial. Under perspective, it important to study proteins that regulate homeostasis cell. Sorcin one most expressed calcium-binding human brain; its overexpression increases endoplasmic reticulum (ER) concentration decreases ER stress heart other...
Leishmaniasis, Chagas disease, and sleeping sickness affect millions of people worldwide lead to the death about 50 000 humans per year. These diseases are caused by kinetoplastids Leishmania, Trypanosoma cruzi, brucei, respectively. parasites share many general features, including gene conservation, high amino acid identity among proteins, presence subcellular structures as glycosomes kinetoplastid, genome architecture, that may make drug development family specific, rather than...
Trypanothione reductase (TR) is a key enzyme that catalyzes the reduction of trypanothione, an antioxidant dithiol protects Trypanosomatid parasites from oxidative stress induced by mammalian host defense systems. TR considered attractive target for development novel anti-parasitic agents as it essential parasite survival but has no close homologue in humans. We report here identification spiro-containing derivatives inhibitors Trypanosoma brucei (TbTR), responsible Human African...
Pyridoxal 5'-phosphate (PLP), the catalytically active form of vitamin B6, plays a pivotal role in metabolism as an enzyme cofactor. PLP is very reactive molecule and can be toxic unless its intracellular concentration finely regulated. In Escherichia coli, formation catalyzed by pyridoxine oxidase (PNPO), homodimeric FMN-dependent that responsible for last step biosynthesis also involved salvage pathway. We have recently observed E. coli PNPO undergoes allosteric feedback inhibition PLP,...
Leishmania spp. are responsible for up to 1 million new cases each year. The current therapeutic arsenal against is largely inadequate, and there an urgent need better drugs. Trypanothione reductase (TR) represents a druggable target since it essential the parasite not shared by human host. Here, we report optimization of novel class potent selective LiTR inhibitors realized through concerted effort involving X-ray crystallography, synthesis, structure–activity relationship (SAR)...
Cancer Drug Resistance is an open access journal, focusing on pharmacological aspects of drug resistance and its reversal, molecular mechanisms classes, etc. Both clinical experimental in cancer are included.
Huntington disease (HD) is a devastating and presently untreatable neurodegenerative characterized by progressively disabling motor mental manifestations. The sigma-1 receptor (σ1R) protein expressed in the central nervous system, whose 3D structure has been recently determined X-ray crystallography agonists have shown to neuroprotective activity diseases. To identify therapeutic agents against HD, we implemented drug repositioning strategy consisting of: (i) Prediction of ability...
The σ1 receptor (σ1-R) is an enigmatic endoplasmic reticulum resident transmembrane protein implicated in a variety of central nervous system disorders and whose agonists have neuroprotective activity. In spite σ1-R's physio-pathological pharmacological importance, two the most important features required to fully understand σ1-R function, namely endogenous ligand(s) molecular mechanism ligand access binding site, not yet been unequivocally determined. this work, we performed dynamics (MD)...
<h3>Background</h3> Huntington's Disease (HD) is a devastating and presently untreatable neurodegenerative disease, characterized by progressively disabling motor mental manifestations. Sigma-1 receptor (σ1R), whose 3D structure has been recently determined X-ray crystallography, expressed in the central nervous system, σ1R agonists have shown to possess neuroprotective activity diseases. <h3>Aims</h3> Our overall aim exploit for HD therapy. <h3>Methods</h3> We are integrating computational...