Search Results - "La Regina, Giuseppe"
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RS-5645 attenuates inflammatory cytokine storm induced by SARS-CoV-2 spike protein and LPS by modulating pulmonary microbiota
Published in International journal of biological sciences (01-01-2021)“…An inflammatory cytokine storm is considered an important cause of death in severely and critically ill COVID-19 patients, however, the relationship between…”
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2
Looking for an Active Conformation of the Future HIV Type-1 Non-Nucleoside Reverse Transcriptase Inhibitors
Published in Antiviral Chemistry and Chemotherapy (01-08-2010)“…HIV type-1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs) are key drugs of highly active antiretroviral therapy (HAART) in the clinical…”
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Book Review Journal Article -
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Venting-while-Heating Microwave-Assisted Synthesis of 3-Arylthioindoles
Published in ACS combinatorial science (09-04-2012)“…We report the first example of venting-while-heating microwave-assisted synthesis of a small library of 3-arylthioindoles. Compounds were prepared in excellent…”
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4
Targeting the Interaction between the SH3 Domain of Grb2 and Gab2
Published in Cells (Basel, Switzerland) (07-11-2020)“…Gab2 is a scaffolding protein, overexpressed in many types of cancers, that plays a key role in the formation of signaling complexes involved in cellular…”
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Targeting CBP and p300: Emerging Anticancer Agents
Published in Molecules (Basel, Switzerland) (24-09-2024)“…CBP and p300 are versatile transcriptional co-activators that play essential roles in regulating a wide range of signaling pathways, including Wnt/β-catenin,…”
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Metabolic Rewiring in Cancer: Small Molecule Inhibitors in Colorectal Cancer Therapy
Published in Molecules (Basel, Switzerland) (01-05-2024)“…Alterations in cellular metabolism, such as dysregulation in glycolysis, lipid metabolism, and glutaminolysis in response to hypoxic and low-nutrient…”
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Emerging Therapeutic Agents for Colorectal Cancer
Published in Molecules (Basel, Switzerland) (09-12-2021)“…There are promising new therapeutic agents for CRC patients, including novel small-molecule inhibitors and immune checkpoint blockers. We focused on emerging…”
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Emerging Direct Targeting β-Catenin Agents
Published in Molecules (Basel, Switzerland) (10-11-2022)“…Aberrant accumulation of β-catenin in the cell nucleus as a result of deregulation of the Wnt/β-catenin pathway is found in various types of cancer. Direct…”
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Recent Advances in Drug Discovery for Triple-Negative Breast Cancer Treatment
Published in Molecules (Basel, Switzerland) (01-11-2023)“…Triple-negative breast cancer (TNBC) is one of the most heterogeneous and aggressive breast cancer subtypes with a high risk of death on recurrence. To date,…”
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Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments
Published in Scientific reports (20-10-2015)“…A Cannabinoid Receptor 1 (CB 1 ) binding site for the selective allosteric modulator ORG27569 is here identified through an integrate approach of consensus…”
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Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity profile
Published in Bioorganic & medicinal chemistry (01-08-2009)“…New substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized by replacing the 2,4-dichlorobenzyl and cyclohexyl moieties at the…”
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12
A Novel Validated UHPLC Method for the Estimation of Rosuvastatin and Its Complete Impurity Profile in Tablet Formulations
Published in Molecules (Basel, Switzerland) (01-01-2023)“…A key step in the development of medicinal products is the research and validation of selective and sensitive analytical methods for the control of impurities…”
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Mechanism of Interaction of Novel Indolylarylsulfone Derivatives with K103N and Y181I Mutant HIV-1 Reverse Transcriptase in Complex with its Substrates
Published in Antiviral chemistry & chemotherapy (01-12-2011)“…Background: Novel indolylarylsulfones (lASs), designed through rational structure-based molecular modelling and docking approaches, have been recently…”
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Biological evaluation of [4‐(4‐aminophenyl)‐1‐(4‐fluorophenyl)‐1 H ‐pyrrol‐3‐yl](3,4,5‐trimethoxyphenyl)methanone as potential antineoplastic agent in 2D and 3D breast cancer models
Published in Archiv der Pharmazie (Weinheim) (01-10-2023)“…Abstract Targeting tubulin polymerization and depolymerization represents a promising approach to treat solid tumors. In this study, we investigated the…”
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Small Molecule Inhibitors of KDM5 Histone Demethylases Increase the Radiosensitivity of Breast Cancer Cells Overexpressing JARID1B
Published in Molecules (Basel, Switzerland) (04-05-2019)“…: KDM5 enzymes are H3K4 specific histone demethylases involved in transcriptional regulation and DNA repair. These proteins are overexpressed in different…”
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β-catenin knockdown promotes NHERF1-mediated survival of colorectal cancer cells: implications for a double-targeted therapy
Published in Oncogene (01-06-2018)“…Nuclear activated β -catenin plays a causative role in colorectal cancers (CRC) but remains an elusive therapeutic target. Using human CRC cells harboring…”
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Toward Highly Potent Cancer Agents by Modulating the C‑2 Group of the Arylthioindole Class of Tubulin Polymerization Inhibitors
Published in Journal of medicinal chemistry (10-01-2013)“…New arylthioindole derivatives having different cyclic substituents at position 2 of the indole were synthesized as anticancer agents. Several compounds…”
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Sulfonamide Inhibitors of β‐Catenin Signaling as Anticancer Agents with Different Output on c‐MYC
Published in ChemMedChem (03-12-2020)“…The Wnt/β‐catenin pathway is often found deregulated in cancer. The aberrant accumulation of β‐catenin in the cell nucleus results in the development of…”
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Targeting PDZ domains as potential treatment for viral infections, neurodegeneration and cancer
Published in Biology direct (12-10-2021)“…The interaction between proteins is a fundamental event for cellular life that is generally mediated by specialized protein domains or modules. PDZ domains are…”
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AN IMPROVED SYNTHESIS OF ETHYL 5-CHLORO-4-FLUORO-1H-INDOLE-2-CARBOXYLATE
Published in Organic preparations and procedures international (01-04-2008)Get full text
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