Elena Dreassi
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View article: Optimization of 2,3-dihydrophthalazine-1,4-dione PARP inhibitor scaffold for nanomolar potency and specificity towards human PARP10
Optimization of 2,3-dihydrophthalazine-1,4-dione PARP inhibitor scaffold for nanomolar potency and specificity towards human PARP10 Open
PARP10 is a potential drug target due to its overexpression in several cancer types and its roles in DNA repair mechanisms and tumorigenesis. In this study, we performed an optimization campaign on our earlier compounds based on a 2,3-dihy…
View article: Fluoromethylcarnitine, a novel inhibitor of trimethylamine levels in trimethylaminuria and trimethylamine N-oxide related disorders
Fluoromethylcarnitine, a novel inhibitor of trimethylamine levels in trimethylaminuria and trimethylamine N-oxide related disorders Open
Excessive production of trimethylamine (TMA) by the gut microbiota leads to increased concentrations of TMA or trimethylamine N-oxide (TMAO) in the bloodstream, which is associated with health risks. High levels of TMAO have been linked to…
View article: Harnessing prebiotic formamide chemistry: a novel platform for antiviral exploration
Harnessing prebiotic formamide chemistry: a novel platform for antiviral exploration Open
View article: Evaluation of Antitumoral Activity in a 3D Cell Model of a Src Inhibitor Prodrug for Glioblastoma Treatment
Evaluation of Antitumoral Activity in a 3D Cell Model of a Src Inhibitor Prodrug for Glioblastoma Treatment Open
Background: Three-dimensional (3D) cell models may bridge the gap between two-dimensional (2D) cell cultures and animal models. Technical advances have led to the development of 3D-bioprinted cell models, characterized by greater reproduci…
View article: Deciphering the landscape of allosteric glutaminase 1 inhibitors as anticancer agents
Deciphering the landscape of allosteric glutaminase 1 inhibitors as anticancer agents Open
Glutamine is the second most utilised energy source after glucose for cancer cells to support their proliferation and survival. Glutaminase 1 (GLS1) is the rate-limiting enzyme during the glutaminolysis pathway and thus represents a promis…
View article: Insects as Source of Nutraceuticals with Antioxidant, Antihypertensive, and Antidiabetic Properties: Focus on the Species Approved in Europe up to 2024
Insects as Source of Nutraceuticals with Antioxidant, Antihypertensive, and Antidiabetic Properties: Focus on the Species Approved in Europe up to 2024 Open
Insects represent a traditional food in different parts of the world, where eating insects is not only related to nutrition, but also results from a variety of sociocultural customs. Insects’ nutritional profiles typically vary by species.…
View article: Light-mediated activation/deactivation control and in vitro ADME-Tox profiling of a donepezil-like Dual AChE/MAO-B Inhibitor
Light-mediated activation/deactivation control and in vitro ADME-Tox profiling of a donepezil-like Dual AChE/MAO-B Inhibitor Open
The possibility to control the effects of drugs in time and space represents an ideal condition for developing safer and more personalized therapies against different disorders. In this context, photopharmacology has paved the way for the …
View article: Exploitation of the Nutraceutical Potential of the Infesting Seaweed Chaetomorpha linum as a Yellow Mealworms’ Feed: Focus on Nutrients and Antioxidant Activity
Exploitation of the Nutraceutical Potential of the Infesting Seaweed Chaetomorpha linum as a Yellow Mealworms’ Feed: Focus on Nutrients and Antioxidant Activity Open
According to the Sustainable Blue Economy Communication, the Farm to Fork Strategy, and the European Green Deal, novel business models supporting the use of resources from oceans and seas are of primary importance. Interestingly, several i…
View article: Upcycling Milk Industry Byproducts into Tenebrio molitor Larvae: Investigation on Fat, Protein, and Sugar Composition
Upcycling Milk Industry Byproducts into Tenebrio molitor Larvae: Investigation on Fat, Protein, and Sugar Composition Open
Edible insects represent a growing sector of the food industry and have a low carbon footprint. Noteworthy, insects can upcycle different leftovers and byproducts into high-quality nutrients. Herein, the larvae of the edible insect Tenebri…
View article: Applying molecular hybridization to design a new class of pyrazolo[3,4-d]pyrimidines as Src inhibitors active in hepatocellular carcinoma
Applying molecular hybridization to design a new class of pyrazolo[3,4-d]pyrimidines as Src inhibitors active in hepatocellular carcinoma Open
Hepatocellular carcinoma (HCC) is the most common type of liver solid tumor and the second leading cause of cancer-related deaths worldwide. Although new treatment options have been recently approved, the development of tumor resistance an…
View article: Exploiting the bile acid binding protein as transporter of a Cholic Acid/Mirin bioconjugate for potential applications in liver cancer therapy
Exploiting the bile acid binding protein as transporter of a Cholic Acid/Mirin bioconjugate for potential applications in liver cancer therapy Open
Bioconjugation is one of the most promising strategies to improve drug delivery, especially in cancer therapy. Biomolecules such as bile acids (BAs) have been intensively explored as carriers, due to their peculiar physicochemical properti…
View article: Novel multitarget directed ligands inspired by riluzole: A serendipitous synthesis of substituted benzo[b][1,4]thiazepines potentially useful as neuroprotective agents
Novel multitarget directed ligands inspired by riluzole: A serendipitous synthesis of substituted benzo[b][1,4]thiazepines potentially useful as neuroprotective agents Open
View article: Optimization of potent, broad-spectrum, and specific anti-influenza compounds targeting RNA polymerase PA-PB1 heterodimerization
Optimization of potent, broad-spectrum, and specific anti-influenza compounds targeting RNA polymerase PA-PB1 heterodimerization Open
View article: Infesting Seaweeds as a Novel Functional Food: Analysis of Nutrients, Antioxidants and ACE Inhibitory Effects
Infesting Seaweeds as a Novel Functional Food: Analysis of Nutrients, Antioxidants and ACE Inhibitory Effects Open
Globalization and climate change are both contributing to an increase in the number of potentially invasive algae in coastal areas. In terms of biodiversity and financial losses, the invasiveness of algae has become a significant issue in …
View article: Phytochemical Composition, Anti-Inflammatory Property, and Anti-Atopic Effect of Chaetomorpha linum Extract
Phytochemical Composition, Anti-Inflammatory Property, and Anti-Atopic Effect of Chaetomorpha linum Extract Open
Utilizing plant-based resources, particularly their by-products, aligns with sustainability principles and circular bioeconomy, contributing to environmental preservation. The therapeutic potential of plant extracts is garnering increasing…
View article: Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy
Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy Open
The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques t…
View article: A Drug Discovery Approach to a Reveal Novel Antioxidant Natural Source: The Case of Chestnut Burr Biomass
A Drug Discovery Approach to a Reveal Novel Antioxidant Natural Source: The Case of Chestnut Burr Biomass Open
Currently, many environmental and energy-related problems are threatening the future of our planet. In October 2022, the Worldmeter recorded the world population as 7.9 billion people, estimating that there will be an increase of 2 billion…
View article: Serendipitous Identification of Azine Anticancer Agents by a Privileged Scaffold Morphing Strategy
Serendipitous Identification of Azine Anticancer Agents by a Privileged Scaffold Morphing Strategy Open
The use of privileged scaffolds as starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques tha…
View article: Identification of Novel Non-Nucleoside Inhibitors of Zika Virus NS5 Protein Targeting MTase Activity
Identification of Novel Non-Nucleoside Inhibitors of Zika Virus NS5 Protein Targeting MTase Activity Open
Zika virus (ZIKV) is a positive-sense single-stranded virus member of the Flaviviridae family. Among other arboviruses, ZIKV can cause neurological disorders such as Guillain Barré syndrome, and it can have congenital neurological manifest…
View article: An Update on Antibacterial Alkylguanidino Ureas Design of New Derivatives, Synergism with Colistin and Data Analysis of the Whole Library
An Update on Antibacterial Alkylguanidino Ureas Design of New Derivatives, Synergism with Colistin and Data Analysis of the Whole Library Open
View article: THE REPLACEMENT OF FLOUR-BASED FEED WITH PELLETS REDUCES DUSTINESS AND IMPROVES TENEBRIO MOLITOR BREEDERS’ SAFETY
THE REPLACEMENT OF FLOUR-BASED FEED WITH PELLETS REDUCES DUSTINESS AND IMPROVES TENEBRIO MOLITOR BREEDERS’ SAFETY Open
Tenebrio molitor larvae (TML) are a novel food, recently approved for human consumption in Europe. Their high content of proteins and polyunsaturated fatty acids make them a healthy source of nutrients, with potential applications in cardi…
View article: Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors
Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors Open
View article: Sweet Cherry Extract as Permeation Enhancer of Tyrosine Kinase Inhibitors: A Promising Prospective for Future Oral Anticancer Therapies
Sweet Cherry Extract as Permeation Enhancer of Tyrosine Kinase Inhibitors: A Promising Prospective for Future Oral Anticancer Therapies Open
Although patients would rather oral therapies to injections, the gastrointestinal tract’s low permeability makes this method limiting for most compounds, including anticancer drugs. Due to their low bioavailability, oral antitumor therapie…
View article: Targeting GLI1 and GLI2 with small molecule inhibitors to suppress GLI-dependent transcription and tumor growth
Targeting GLI1 and GLI2 with small molecule inhibitors to suppress GLI-dependent transcription and tumor growth Open
Aberrant activation of Hedgehog (HH) signaling in cancer is the result of genetic alterations of upstream pathway components (canonical) or other oncogenic mechanisms (noncanonical), that ultimately concur to activate the zinc-finger trans…
View article: Brevundimonas aurantiaca M3d10, Isolated from the Olive Fly, Produces Hydroxylated Astaxanthin
Brevundimonas aurantiaca M3d10, Isolated from the Olive Fly, Produces Hydroxylated Astaxanthin Open
In recent years, the exploitation of bacteria for the production of carotenoids has become of great interest as a sustainable alternative to chemical synthesis, which is expensive and technically challenging. This study contributes to the …
View article: Progress towards Adjuvant Development: Focus on Antiviral Therapy
Progress towards Adjuvant Development: Focus on Antiviral Therapy Open
In recent decades, vaccines have been extraordinary resources to prevent pathogen diffusion and cancer. Even if they can be formed by a single antigen, the addition of one or more adjuvants represents the key to enhance the response of the…
View article: Discovery and Optimization of a Novel Macrocyclic Amidinourea Series Active as Acidic Mammalian Chitinase Inhibitors
Discovery and Optimization of a Novel Macrocyclic Amidinourea Series Active as Acidic Mammalian Chitinase Inhibitors Open
Our research group has been involved for a long time in the development of macrocyclic amidinoureas (MCAs) as antifungal agents. The mechanistic investigation drove us to perform an in silico target fishing study, which allowed the …
View article: Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme
Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme Open
The therapeutic use of tyrosine kinase inhibitors (TKIs) represents one of the successful strategies for the treatment of glioblastoma (GBM). Pyrazolo[3,4-d]pyrimidines have already been reported as promising small molecules active as c-Sr…
View article: Tenebrio molitor as a Simple and Cheap Preclinical Pharmacokinetic and Toxicity Model
Tenebrio molitor as a Simple and Cheap Preclinical Pharmacokinetic and Toxicity Model Open
The progression of drugs into clinical phases requires proper toxicity assessment in animals and the correct identification of possible metabolites. Accordingly, different animal models are used to preliminarily evaluate toxicity and biotr…
View article: [1,2,4]Triazolo[3,4- <i>b</i> ]benzothiazole Scaffold as Versatile Nicotinamide Mimic Allowing Nanomolar Inhibition of Different PARP Enzymes
[1,2,4]Triazolo[3,4- <i>b</i> ]benzothiazole Scaffold as Versatile Nicotinamide Mimic Allowing Nanomolar Inhibition of Different PARP Enzymes Open
We report [1,2,4]triazolo[3,4-b]benzothiazole (TBT) as a new inhibitor scaffold, which competes with nicotinamide in the binding pocket of human poly- and mono-ADP-ribosylating enzymes. The binding mode was studied through analogues…