Synthesis of 1,10-Phenanthroline-2,9-bistriazoles: Evaluation as G-Quadruplex Binders and Anti-Tumor Activity.

Novel 1,10-phenanthroline-2,9-bistriazoles derivatives have been synthesized by copper-catalyzed azide/alkyne cycloaddition reactions and assessed for their ability to bind and stabilize G-quadruplex (G4) structures. Ten novel compounds were evaluated using Förster resonance energy transfer (FRET) melting, circular dichroism (CD), and fluorescence spectroscopy on several G4 sequences. Biophysical characterization led to the identification of compounds 4 a, 4 b, and 5 b as good G4 ligands of KRAS G4 sequences.

Combining graph neural networks and transformers for few-shot nuclear receptor binding activity prediction.

Nuclear receptors (NRs) play a crucial role as biological targets in drug discovery. However, determining which compounds can act as endocrine disruptors and modulate the function of NRs with a reduced amount of candidate drugs is a challenging task. Moreover, the computational methods for NR-binding activity prediction mostly focus on a single receptor at a time, which may limit their effectiveness.

Proteomic Profile of Endometrial Cancer: A Scoping Review.

Proteomics can be a robust tool in protein identification and regulation, allowing the discovery of potential biomarkers. In clinical practice, the management of endometrial cancer can be challenging. Thus, identifying promising markers could be beneficial, helping both in diagnosis and prognostic stratification, even predicting the response to therapy.

Design of experiment (DoE) of mucoadhesive valproic acid-loaded nanostructured lipid carriers (NLC) for potential nose-to-brain application.

Epilepsy is a highly prevalent neurological disease and valproic acid (VPA) is used as a first-line chronic treatment. However, this drug has poor oral bioavailability, which requires the administration of high doses, resulting in adverse effects. Alternative routes of VPA administration have therefore been investigated, such as the nose-to-brain route, which allows the drug to be transported directly from the nasal cavity to the brain.

A Hybrid GNN Approach for Improved Molecular Property Prediction.

The development of new drugs is a vital effort that has the potential to improve human health, well-being and life expectancy. Molecular property prediction is a crucial step in drug discovery, as it helps to identify potential therapeutic compounds. However, experimental methods for drug development can often be time-consuming and resource-intensive, with a low probability of success.

Unlocking the Bioactive Potential and Exploring Novel Applications for Portuguese Endemic .

The infusion of , an endemic Portuguese plant, is traditionally used to treat various infections and disorders. This study aimed to assess its chemical profile by HPLC-DAD-ESI-MS and validate its anti-inflammatory potential. In addition, the antioxidant capacity and effects on wound healing, lipogenesis, melanogenesis, and cellular senescence, all processes in which a dysregulated inflammatory response plays a pivotal role, were unveiled.

Connexin43 promotes exocytosis of damaged lysosomes through actin remodelling.

A robust and efficient cellular response to lysosomal membrane damage prevents leakage from the lysosome lumen into the cytoplasm. This response is understood to happen through either lysosomal membrane repair or lysophagy. Here we report exocytosis as a third response mechanism to lysosomal damage, which is further potentiated when membrane repair or lysosomal degradation mechanisms are impaired.

Validation of a new sampler for radon gas measurements in surface water.

Radon gas (Rn-222) in water poses health risks due to radiation exposure, yet it's also an important tracer for studying natural systems. Sampling procedures for Rn-222 analysis are very sensitive to potential losses of the gas to the atmosphere. It requires a well-defined and properly validated protocol to ensure accuracy and reliability.

Rational formulation and industrial manufacturing of lipid-based complex injectables: Landmarks and trends.

Lipid-based complex injectables are renowned for their effectiveness in delivering drugs, with many approved products. While significant strides have been made in formulating nanosystems for small molecular weight drugs, a pivotal breakthrough emerged with the recognition of lipid nanoparticles as a promising platform for delivering nucleic acids. This finding has paved the way for tackling long-standing challenges in molecular and delivery aspects (e.

Plant-derived and dietary phenolic cinnamic acid derivatives: Anti-inflammatory properties.

Cinnamic acids are aromatic acids primarily found in plants and plant-derived food. Phenolic cinnamic acids, with one or more hydroxyl groups in the aromatic ring, often contribute to the biological activities attributed to these compounds. The presence of hydroxyl groups and a carboxyl group makes cinnamic acids very hydrophilic, preventing them from crossing biological membranes and exerting their biological activities.

Scattering approaches to unravel protein solution behaviors in ionic liquids and deep eutectic solvents: From basic principles to recent developments.

Proteins in ionic liquids (ILs) and deep eutectic solvents (DESs) have gained significant attention due to their potential applications in various fields, including biocatalysis, bioseparation, biomolecular delivery, and structural biology. Scattering approaches including dynamic light scattering (DLS) and small-angle X-ray and neutron scattering (SAXS and SANS) have been used to understand the solution behavior of proteins at the nanoscale and microscale. This review provides a thorough exploration of the application of these scattering techniques to elucidate protein properties in ILs and DESs.

Effectiveness of photodynamic therapy on treatment response and survival in patients with recurrent oral squamous cell carcinoma: A systematic review.

Background: This systematic review assessed the effectiveness of photodynamic therapy (PDT) in patients with recurrent oral squamous cell carcinoma (OSCC).

Methods: Clinical studies on recurrent OSCC treated with PDT alone were included. Combined treatment strategies were excluded.

Development and validation of an HPLC-DAD method for the quantification of cannabigerol, cannabidiol, cannabinol and cannabichromene in human plasma and mouse matrices.

Cannabigerol, cannabidiol, cannabinol and cannabichromene are non-psychoactive phytocannabinoids, highly present in , for which numerous therapeutical applications have been described. However, additional pre-clinical and clinical data, including toxicopharmacokinetic and pharmacodynamic studies, remain required to support their use in clinical practice and new therapeutic applications. To support these studies, a new high performance liquid chromatography technique (HPLC) with diode-array detection (DAD) was developed and validated to quantify these cannabinoids in human plasma and mouse matrices.

Animal model for in-vivo Nuclear Cataract. Lens hardness and elasticity assessment.

Age-related cataract is the most frequent cause of blindness in the world being responsible for 48% of blindness and affecting more than 10% of the working population. Currently there is no objective data of the lens biomechanical properties so the process by which the cataract affects the lens's properties (e.g.

Computed tomography imaging in preprocedural planning of transcatheter valvular heart interventions.

Cardiac Computed Tomography (CCT) has become a reliable imaging modality in cardiology providing robust information on the morphology and structure of the heart with high temporal and isotropic spatial resolution. For the past decade, there has been a paradigm shift in the management of valvular heart disease since previously unfavorable candidates for surgery are now provided with less-invasive interventions. Transcatheter heart valve interventions provide a real alternative to medical and surgical management and are often the only treatment option for valvular heart disease patients.

People's experiences of their involvement in nursing care: a systematic review protocol.

Background: People's involvement and participation in their own care are the essential basis of nursing care. This phenomenon can be characterised as an approach based on the integration of the person's values, beliefs, and preferences during nursing care. This process contributes to improve quality of care, improve satisfaction levels, and result in a better experience for people receiving care.

Development of a new affinity maturation protocol for the construction of an internalizing anti-nucleolin antibody library.

Over the last decades, monoclonal antibodies have substantially improved the treatment of several conditions. The continuous search for novel therapeutic targets and improvements in antibody's structure, demands for a constant optimization of their development. In this regard, modulation of an antibody's affinity to its target has been largely explored and culminated in the discovery and optimization of a variety of molecules.

Steroidal epoxides as anticancer agents in lung, prostate and breast cancers: The case of 1,2-epoxysteroids.

Cancer continues to be a serious threat to human health worldwide. Lung, prostate and triple-negative breast cancers are amongst the most incident and deadliest cancers. Steroidal compounds are one of the most diversified therapeutic classes of compounds and they were proven to be efficient against several types of cancer.

Indoleamine 2,3-dioxygenase (IDO1) - Can dendritic cells and monocytes expressing this moonlight enzyme change the phase of Parkinson's Disease?

Parkinson's Disease (PD) is the second most common neurodegenerative disease where central and peripheral immune dysfunctions have been pointed out as a critical component of susceptibility and progression of this disease. Dendritic cells (DCs) and monocytes are key players in promoting immune response regulation and can induce the enzyme indoleamine 2,3-dioxygenase 1 (IDO1) under pro-inflammatory environments. This enzyme with catalytic and signaling activity supports the axis IDO1-KYN-aryl hydrocarbon receptor (AhR), promoting disease-specific immunomodulatory effects.

Expression and Function of Connexins in Extracellular Vesicles.

Extracellular vesicles (EVs) are recognized as major vehicles for exchange of information across distant cells and tissues, which have been extensively explored for diagnosis and therapeutic purposes. The presence of multiple connexin (Cx) proteins has been described in EVs, where they might facilitate EV-cell communication. However, quantitative changes in Cx levels and functional assessment of Cx channels have only been established for Cx43.