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Topic Review
Binding of Cholesterol to GPCRs
G-protein coupled receptors (GPCRs) are membrane proteins that convey extracellular signals to the cellular milieu. They represent a target for more than 30% of currently marketed drugs.
  • 1.3K
  • 27 Mar 2021
Topic Review
Multiple Functions of Melatonin in the Military Setting
Melatonin is a technique that is being increasingly employed to manage growing psycho-physical loads. In this context, melatonin, a pleotropic and regulatory molecule, has a potential preventive and therapeutic role in maintaining the operational efficiency of military personnel. In battlefield conditions in particular, the time to treatment after an injury is often a major issue since the injured may not have immediate access to medical care. Any drug that would help to stabilize a wounded individual, especially if it can be immediately administered (e.g., per os) and has a very high safety profile over a large range of doses (as melatonin does) would be an important asset to reduce morbidity and mortality.
  • 1.3K
  • 06 Feb 2023
Topic Review
Nanosystems for Brain Drug Delivery
Antipsychotic drugs have numerous disabling side effects, and many are lipophilic, making them hard to formulate at high strength. Incorporating them into nanometric emulsions can increase their solubility, protect them from degradation, and increase their brain delivery, being a promising strategy to overcome the current treatment gap.
  • 1.3K
  • 09 Nov 2022
Topic Review
β-Naphthoflavone, Ethanol Reverse Mitochondrial Dysfunction
The 1-methyl-4-phenylpyridinium (MPP+) is a parkinsonian-inducing toxin that promotes neurodegeneration of dopaminergic cells by directly targeting complex I of mitochondria. Recently, it was reported that some Cytochrome P450 (CYP) isoforms, such as CYP 2D6 or 2E1, may be involved in the development of this neurodegenerative disease. In order to study a possible role for CYP induction in neurorepair, we designed an in vitro model where undifferentiated neuroblastoma SH-SY5Y cells were treated with the CYP inducers β-naphthoflavone (βNF) and ethanol (EtOH) before and during exposure to the parkinsonian neurotoxin, MPP+. The toxic effect of MPP+ in cell viability was rescued with both βNF and EtOH treatments. We also report that this was due to a decrease in reactive oxygen species (ROS) production, restoration of mitochondrial fusion kinetics, and mitochondrial membrane potential. These treatments also protected complex I activity against the inhibitory effects caused by MPP+, suggesting a possible neuroprotective role for CYP inducers. These results bring new insights into the possible role of CYP isoenzymes in xenobiotic clearance and central nervous system homeostasis.
  • 1.3K
  • 02 Nov 2020
Topic Review
Cardiac Fibrosis and Fibroblasts
Cardiac fibrosis is the excess deposition of extracellular matrix (ECM), such as collagen.
  • 1.3K
  • 23 Jul 2021
Topic Review
Effects of Statins on Cancer via Autophagy
Cancer is one of the main causes of death globally. Most of the molecular mechanisms underlying cancer are marked by complex aberrations that activate the critical cell-signaling pathways that play a pivotal role in cell metabolism, tumor development, cytoskeletal reorganization, and metastasis. The phosphatidylinositol 3-kinase/protein kinase-B/mammalian target of the rapamycin (PI3K/AKT/mTOR) pathway is one of the main signaling pathways involved in carcinogenesis and metastasis. Autophagy, a cellular pathway that delivers cytoplasmic components to lysosomes for degradation, plays a dual role in cancer, as either a tumor promoter or a tumor suppressor, depending on the stage of the carcinogenesis. Statins are the group of drugs of choice to lower the level of low-density lipoprotein (LDL) cholesterol in the blood. Experimental and clinical data suggest the potential of statins in the treatment of cancer. In vitro and in vivo studies have demonstrated the molecular mechanisms through which statins inhibit the proliferation and metastasis of cancer cells in different types of cancer. The anticancer properties of statins have been shown to result in the suppression of tumor growth, the induction of apoptosis, and autophagy.
  • 1.3K
  • 09 Jun 2022
Topic Review
Cutaneous Reactions to Antidiabetic Agents
Diabetes is a common and complex disease affecting multiple organ systems throughout the body. With a consensus in care guidelines emphasizing the importance of glycemic control in determining the disease progression, people with diabetes worldwide have been placed on medication regimens targeting glucose stability from a variety of pathophysiologic pathways. Each of these medications also possesses its own potential for adverse events. 
  • 1.3K
  • 04 Mar 2022
Topic Review
Anthocyanins in Nano-Delivery Systems
Anthocyanins are among the best-known phenolic compounds and possess remarkable biological activities, including antioxidant, anti-inflammatory, anticancer, and antidiabetic effects. Despite their therapeutic benefits, they are not widely used as health-promoting agents due to their instability, low absorption, and, thus, low bioavailability and rapid metabolism in the human body. Research suggests that the application of nanotechnology could increase their solubility and/or bioavailability, and thus their biological potential. 
  • 1.3K
  • 03 Nov 2022
Topic Review
Innovations in Chewable Formulations and 3D Printing
Since their introduction, chewable dosage forms have gained traction due to their ability to facilitate swallowing, especially in paediatric, geriatric and dysphagia patients. Their benefits stretch beyond human use to also include veterinary applications, improving administration and palatability in different animal species. Despite their advantages, current chewable formulations do not account for individualised dosing and palatability preferences. In light of this, three-dimensional (3D) printing, and in particular the semi-solid extrusion technology, has been suggested as a novel manufacturing method for producing customised chewable dosage forms. This advanced approach offers flexibility for selecting patient-specific doses, excipients, and organoleptic properties, which are critical for ensuring efficacy, safety and adherence to the treatment. 
  • 1.3K
  • 07 Sep 2022
Topic Review
Pharmacokinetic Analysis of Ethanol in a Human Study
In the pharmacokinetic analysis of ethanol after oral administration, only single- or two-compartment models are used, but their precision in estimating pharmacokinetic parameters might be insufficient. Pharmacokinetic parameters obtained using pharmacokinetic models differ depending on the type of model used. The estimated pharmacokinetic parameters depend on the type of model used. The classic Widmark model in particular overestimated the fraction of absorbed ethanol from the gastrointestinal system to systemic circulation. 
  • 1.3K
  • 23 Oct 2023
Topic Review
Intravitreal Delivery Systems for Sustained Drug Release
Slow-release delivery systems are needed to ensure long-term sustained treatments for retinal diseases such as age-related macular degeneration and diabetic retinopathy, which are currently treated with anti-angiogenic agents that require frequent intraocular injections. These can cause serious co-morbidities for the patients and are far from providing the adequate drug/protein release rates and required pharmacokinetics to sustain prolonged efficacy.
  • 1.3K
  • 17 May 2023
Topic Review
Antibiotic Resistance in Bronchiectasis
Non-cystic fibrosis bronchiectasis is a chronic disorder in which immune system dysregulation and impaired airway clearance cause mucus accumulation and consequent increased susceptibility to lung infections. The presence of pathogens in the lower respiratory tract causes a vicious circle resulting in impaired mucociliary function, bronchial inflammation, and progressive lung injury. In current guidelines, antibiotic therapy has a key role in bronchiectasis management to treat acute exacerbations and chronic infection and to eradicate bacterial colonization. 
  • 1.3K
  • 17 May 2021
Topic Review
Docking Studies of Recently Synthesized MAO-B Inhibitors
With the significant growth of patients suffering from neurodegenerative diseases (NDs), novel classes of compounds targeting monoamine oxidase type B (MAO-B) are promptly emerging as distinguished structures for the treatment of the latter. As a promising function of computer-aided drug design (CADD), structure-based virtual screening (SBVS) is being heavily applied in processes of drug discovery and development. The utilization of molecular docking, as a helping tool for SBVS, is providing essential data about the poses and the occurring interactions between ligands and target molecules. 
  • 1.3K
  • 13 Jul 2023
Topic Review
Marine Resources for COVID-19 Treatment
Marine resources have significant pharmacological potential in combatting various diseases, such as COVID-19. The wide variety of marine bioactive compounds and their implications are extensive. Micro and macro-organisms produce inorganic polyphosphates, sulfated polysaccharides, Bromotyrosines and many more. These compounds possess unique properties that allow them to combat Sars-Cov-2 infection, proving as efficacious potential therapeutics. Despite the challenges faced, marine organisms serve as a promising avenue for future pharmacological intervention. The present review for the first time highlights marine bioactive compounds, their sources, and their anti-viral mechanisms of action, with a focus on potential COVID-19 treatment.
  • 1.3K
  • 27 Jul 2021
Topic Review
Natural Polypropionates
Natural polypropionates (PPs) are a large subgroup of polyketides constructed by C3-units. One of the main characteristics to distinguish the PPs is the regularly interspaced methyl groups in the polyketide chain or the cyclic polyketide core, which are driven directly from propionate unit or from the acetate-methionine motif.
  • 1.3K
  • 07 Dec 2020
Topic Review
Solution Nuclear Magnetic Resonance
Solution nuclear magnetic resonance (NMR) spectroscopy is a promising tool in drug discovery. Especially, fragment-based drug discovery (FBDD) has benefited a lot from the NMR development. Multiple candidate compounds and FDA-approved drugs derived from FBDD have been developed with the assistance of NMR techniques. NMR has broad applications in different stages of the FBDD process, which includes fragment library construction, hit generation and validation, hit-to-lead optimization and working mechanism elucidation, etc.
  • 1.3K
  • 09 Feb 2021
Topic Review
Antimicrobial/Antiviral Potential of Cannabinoids and Cannabis sativa
Antimicrobial resistance has emerged as a global health crisis and, therefore, new drug discovery is a paramount need. Cannabis sativa contains hundreds of chemical constituents produced by secondary metabolism, exerting outstanding antimicrobial, antiviral, and therapeutic properties.
  • 1.3K
  • 15 Dec 2021
Topic Review
Combination Therapies in Alzheimer’s Disease
Alzheimer’s disease (AD) is the leading cause of dementia worldwide. Until now, available therapeutic agents for AD treatment only provide symptomatic treatment. Since AD pathogenesis is multifactorial, use of a multimodal therapeutic intervention addressing several molecular targets of AD-related pathological processes seems to be the most practical approach to modify the course of AD progression. It has been demonstrated through numerous studies, that the clinical efficacy of combination therapy (CT) is higher than that of monotherapy. It is indeed difficult to combine several pharmacophores into a single molecule.  It is essential to carry out long-duration randomized controlled trials to establish whether CT delays disease progression in early AD stages. Other factors also need to be assessed in CT, such as its potential neuroprotective effects, cost-effectiveness, and a more exhaustive estimation of its potential benefits on the patients at the end-stage of AD.
  • 1.3K
  • 28 Oct 2020
Topic Review
Voltage Gated Ion Channels
Safety Pharmacology is one of the most dynamically developing disciplines, whose objective is to assess the potential risks of improperly conducted pharmacotherapy. Evaluation of a potential risks in the use of a given substance is vital for placing a new medicine on the market. The Organisation for Economic Co-operation and Development (OECD) has issued a number of guidelines for drug safety testing [1, 2]. However, the continuous development of medicine demands the extension and refinement of the test panel that a new molecule must undergo before it can be released for use by patients. Toxic effects of compounds on the most important organs are among the most frequent reasons of elimination of substances from further tests. Additionally, safety tests are also performed for medicines already approved for use. Such trials are required, e.g., to register new indications for "old" drugs.  The above mentioned activities require a suitable identifications of the antitargets which are commonly defined as undesirable molecular targets that play an essential role in the proper functioning of cells. Down modulation of an antitarget results in clinically unacceptable side effects, initiation of disease, or deleterious alterations in disease progression. This results in shorter onset time of the disease, increased disease burden, poorer patient outcome, or decreased survival time.
  • 1.3K
  • 27 Jan 2021
Topic Review
Heterocyclic PPAR Ligands for Potential Therapeutic Applications
The family of nuclear peroxisome proliferator-activated receptors (PPARα, PPARβ/δ, and PPARγ) is a set of ligand-activated transcription factors that regulate different functions in the body. Whereas activation of PPARα is known to reduce the levels of circulating triglycerides and regulate energy homeostasis, the activation of PPARγ brings about insulin sensitization and increases the metabolism of glucose. On the other hand, PPARβ when activated increases the metabolism of fatty acids. Further, these PPARs have been claimed to be utilized in various metabolic, neurological, and inflammatory diseases, neurodegenerative disorders, fertility or reproduction, pain, and obesity.
  • 1.3K
  • 08 Nov 2022
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