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The inflammasome-activating poxvirus peptide IAMP29 promotes antimicrobial and anticancer responses
2024 / Experimental & Molecular MedicinePoxviruses are implicated in a variety of infectious diseases; however, little is known about the molecular mechanisms that underlie the immune response during poxvirus infection. We investigated the function and mechanisms of the monkeypox virus envelope protein (A30L) and its core peptide (IAMP29) during the activation of innate immune responses. The A30L prote...
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Stimuli-Responsive Peptide/siRNA Nanoparticles as a Radiation Sensitizer for Glioblastoma Treatment by Co-Inhibiting RELA/P65 and EGFR
2024 / International Journal of NanomedicinePurpose: To develop a novel approach for increasing radiosensitivity in glioblastoma (GBM) by using targeted nanoparticles to deliver siRNA aimed at silencing the EGFR and RELA/P65 genes, which are implicated in radioresistance. Patients and Methods: We engineered biodegradable, tumor-targeted, self-assembled, and stimuli-responsive peptide nanoparticles for effici...
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Development of a novel N14-substituted antitumor evodiamine derivative with inhibiting heat shock protein 70 in non-small cell lung cancer
2024 / Scientific ReportsNotwithstanding the latest advancements in anticancer therapy, non-small cell lung cancer (NSCLC) remains a prominent contributor to cancer-associated mortality worldwide. Therefore, effective anti-cancer agents are required for the treatment of NSCLC. We previously demonstrated that the natural alkaloid evodiamine efficiently suppressed lung cancer cells and lun...
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Pegylated gold nanoparticles interact with lipid bilayer and human serum albumin and transferrin
2024 / Scientific ReportsGold nanoparticles (AuNPs) are potentially applicable in drug/nucleic acid delivery systems. Low toxicity, high stability, and bioavailability are crucial for the therapeutic use of AuNPs and they are mainly determined by their interactions with proteins and lipids on their route to the target cells. In this work, we investigated the interaction of two pegylated ...
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New LsrK Ligands as AI-2 Quorum Sensing Interfering Compounds against Biofilm Formation
2025 / Journal of Medicinal ChemistryAntimicrobial resistance (AMR) represents a critical global health crisis. An innovative strategy to deal with AMR is to interfere with biofilm formation and bacterial quorum sensing (QS). In this study, newly designed autoinducer-2 (AI-2)-inspired compounds in targeting biofilm-associated infections were evaluated for their ability to inhibit biofilm formation in ...
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An intrinsic mechanism of metabolic tuning promotes cardiac resilience to stress
2024 / EMBO Molecular MedicineDefining the molecular mechanisms underlying cardiac resilience is crucial to find effective approaches to protect the heart. A physiologic level of ROS is produced in the heart by fatty acid oxidation, but stressful events can boost ROS and cause mitochondrial dysfunction and cardiac functional impairment. Melusin is a muscle specific chaperone required for myocar...
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Structure of anellovirus-like particles reveal a mechanism for immune evasion
2024 / Nature CommunicationsAnelloviruses are nonpathogenic viruses that comprise a major portion of the human virome. Despite being ubiquitous in the human population, anelloviruses (ANVs) remain poorly understood. Basic features of the virus, such as the identity of its capsid protein and the structure of the viral particle, have been unclear until now. Here, we use cryogenic electron mic...
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Fibroblast growth receptor 1 is regulated by G-quadruplex in metastatic breast cancer
2024 / Communications BiologyLimiting cellular plasticity is of key importance for the therapeutic targeting of metastatic breast cancer (MBC). Fibroblast growth receptor (FGFR) is a critical molecule in cellular plasticity and potent inhibitors of FGFR enzymatic activity have been developed, but kinase independent functions for this receptor also contribute to MBC progression. Herein, we ev...
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Analysis of the immune response using FTIR spectroscopy in mothers and their newborns with different vaccination schemes for COVID-19
2024 / Scientific ReportsThe SARS-CoV-2 outbreak has provoked more than 6 million deaths worldwide. The scarcity of effective treatments and its virulence converted the vaccines into an essential tool to face it. The most used vaccines were the mRNA, adenovirus vector, and inactivated whole-virus. However, nowadays, infants aged < 6 months are not eligible for any vaccin...
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Backbone-Determined Antiarrhythmic Structure–Activity Relationships for a Mirror Image, Oligomeric Depsipeptide Natural ProductArticle link copied!
2024 / Journal of Medicinal ChemistryCyclic oligomeric depsipeptides (COD) are a structural class within naturally occurring compounds with a wide range of biological activity. Verticilide is a COD (24-membered ring) that was identified by its inhibition of insect ryanodine receptor (RyR). We have since found that the enantiomer of verticilide (ent-verticilide, 1) is a potent inhibitor of mammalian Ry...
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Development and in vitro/in vivo evaluation of a nanosponge formulation loaded with Boswellia carterii oil extracts for the enhanced anti-inflammatory activity for the management of respiratory allergies
2024 / Journal of Pharmaceutical InvestigationIn several nations, it has been known that Boswellia carterii (BC) plants have a long history of usage as an anti-inflammatory medicine. Our current study deals with the study of two different ways of extraction of BC volatile oil and fixed oil as main constituents (Octyl acetate, 46.46% and β-Boswellic acid, 10.21%, respectively), preparation, and evaluation ...
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SU-101 for the removal of pharmaceutical active compounds by the combination of adsorption/photocatalytic processes
2024 / Scientific ReportsPharmaceutical active compounds (PhACs) are some of the most recalcitrant water pollutants causing undesired environmental and human effects. In absence of adapted decontamination technologies, there is an urgent need to develop efficient and sustainable alternatives for water remediation. Metal–organic frameworks (MOFs) have recently emerged as promising c...
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Unlocking Antibacterial Potential: Key-Site-Based Regulation of Antibacterial Spectrum of Peptides
2024 / Journal of Medicinal ChemistryIn the pursuit of combating multidrug-resistant bacteria, antimicrobial peptides (AMPs) have emerged as promising agents; however, their application in clinical settings still presents challenges. Specifically, the exploration of crucial structural parameters that influence the antibacterial spectrum of AMPs and the subsequent development of tailored variants with ...
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Discovery of 2,3-Diaminoindole Derivatives as a Novel Class of NOD Antagonists
2024 / Journal of Medicinal ChemistryNOD1 and NOD2 are members of the pattern recognition receptors involved in the innate immune response. Overactivation of NOD1 is implicated in inflammatory disorders, multiple sclerosis, and cancer cell metastases. NOD1 antagonists would represent valuable pharmacological tools to gain further insight into protein roles, potentially leading to new therapeutic strat...
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Synthesis, anticancer activity, and molecular docking of half-sandwich iron(II) cyclopentadienyl complexes with maleimide and phosphine or phosphite ligands
2024 / Scientific ReportsIn these studies, we designed and investigated the potential anticancer activity of five iron(II) cyclopentadienyl complexes bearing different phosphine and phosphite ligands. All complexes were characterized with spectroscopic analysis viz. NMR, FT–IR, ESI–MS, UV–Vis, fluorescence, XRD (for four complexes) and elemental analyses. For biological...
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