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Topic Review
Cenobamate and Drug-Resistant Epilepsy
Cenobamate (CNB), ([(R)-1-(2-chlorophenyl)-2-(2H-tetrazol-2-yl)ethyl], is a novel tetrazole alkyl carbamate derivative. In November 2019, the Food and Drug Administration approved Xcopri®, marketed by SK Life Science Inc., (Paramus, NJ, USA) for adult focal seizures. The European Medicines Agency approved Ontozry® by Arvelle Therapeutics Netherlands B.V.(Amsterdam, The Neatherlands) in March 2021. Cenobamate is a medication that could potentially change the perspectives regarding the management and prognosis of refractory epilepsy.
  • 995
  • 02 Aug 2023
Topic Review
Endocannabinoid Signaling Pathways
Endocannabinoids play an important role as powerful regulators of synaptic function in the central nervous system where they regulate neural functions and behaviors. As fundamental modulators of synaptic function, endocannabinoids can regulate neural functions such as cognition, motor control, pain, and feeding behavior. The interaction between endogenous or exogenous ligands and endocannabinoid receptors initiates signaling pathways.
  • 994
  • 24 Apr 2023
Topic Review
mRNA, Live-Attenuated/Chimeric and VLP-Based Vaccines
Respiratory syncytial virus (RSV) is an enveloped, negative-sense, single-stranded RNA virus causing seasonal infections in a biphasic age distribution, affecting more frequently children until the age of 2 years with a higher frequency across the age spectrum from 6 weeks to 6 months, as well as older adults due to the reduction of immunity. 
  • 993
  • 03 Nov 2023
Topic Review
GPR21 Inhibition
GPR21 is a constitutively active, orphan, Gq-protein-coupled receptor, with in vivo studies suggesting its involvement in the insulin resistance development.
  • 992
  • 11 Nov 2021
Topic Review
Fungal–Fungal Co-Culture for Discovery of New Secondary Metabolites
Fungi are an important and prolific source of secondary metabolites (SMs) with diverse chemical structures and a wide array of biological properties. Fungal–fungal co-culture is the major source of new SMs and consists of two types including liquid state fermentation (LSF) and solid state fermentation (SSF). Potato dextrose broth (PDB) and rice are the most common co-culture media for fungal LSF and SSF, respectively.
  • 992
  • 24 Nov 2023
Topic Review
A Novel, Pan-PDE Inhibitor From the Group of 7,8-Disubstituted Purine-2,6-Dione Derivatives
Phosphodiesterases (PDEs) inhibitors are currently a widespread and extensively studied group of anti-inflammatory and anti-fibrotic compounds which may find use in the treatment of numerous lung diseases, including asthma and chronic obstructive pulmonary disease. Several PDE inhibitors are currently in clinical development, and some of them, e.g. roflumilast, are already recommended for clinical use. Due to numerous reports indicating that elevated intracellular adenosine 3’,5’-cyclic monophosphate (cAMP) levels may contribute to alleviation of inflammation and airway fibrosis, new and effective PDE inhibitors are constantly being sought. Recently, a group of 7,8-disubstituted purine-2,6-dione derivatives, representing novel and prominent pan-PDE inhibitors has been synthesized. Some of them were reported to modulate transient receptor potential ankyrin 1 (TRPA1) ion channels as well. Compound 145 (4-(8-butoxy-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(5-(tert-butyl)-2-hydroxyphenyl)butanamide) – a pan-PDE inhibitor and a weak TRPA1 modulator inhibited fibroblast to myofibroblasts transition (FMT) as well as MRC-5 human lung fibroblasts proliferation, migration, and contraction. The effect of this compound appeared to depend mainly on its strong PDE inhibitory properties, and not on its effects on TRPA1 modulation. The strong anti-remodelling effects of 145 required activation of the cAMP/protein kinase A/CREB pathway leading to inhibition of transforming growth factor type β1 (TGF-β1) and Smad-dependent signalling in MRC-5 cells.
  • 987
  • 09 Sep 2021
Topic Review
Antifungal Drugs against Paracoccidioidomycosis
Paracoccidioidomycosis is a neglected disease that causes economic and social impacts, mainly affecting people of certain social segments, such as rural workers. The limitations of antifungals, such as toxicity, drug interactions, restricted routes of administration, and the reduced bioavailability in target tissues, have become evident in clinical settings. These factors, added to the fact that Paracoccidioidomycosis (PCM) therapy is a long process, lasting from months to years, emphasize the need for the research and development of new molecules.
  • 987
  • 16 Dec 2020
Topic Review
BPSD and Antipsychotics
Behavioral and psychological symptoms (BPSD) frequently occur during the disease progression; to treat agitation, aggressiveness, delusions and hallucinations, the use of antipsychotic drugs should be limited, due to their safety issues.
  • 986
  • 11 Oct 2021
Topic Review
Induced Tissue-Specific Stem Cells (iTSCs)
Induced tissue-specific stem cells (iTSCs) are partially reprogrammed cells which have an intermediate state, such as progenitors or stem cells. They originate from the de-differentiation of differentiated somatic cells into pluripotent stem cells, such as induced pluripotent stem cells (iPSCs) and embryonic stem cells (ESCs), or from the differentiation of undifferentiated cells. They show a limited capacity to differentiate and a morphology similar to that of somatic cell stem cells present in tissues, but distinct from that of iPSCs and ESCs. iTSCs can be generally obtained 7 to 10 days after reprogramming of somatic cells with Yamanaka’s factors, and their fibroblast-like morphology remains unaltered. iTSCs can also be obtained directly from iPSCs cultured under conditions allowing cellular differentiation. In this case, to effectively induce iTSCs, additional treatment is required, as exemplified by the conversion of iPSCs into naïve iPSCs. iTSCs can proliferate continuously in vitro, but when transplanted into immunocompromised mice, they fail to generate solid tumors (teratomas), implying loss of tumorigenic potential. The low tendency of iTSCs to elicit tumors is beneficial, especially considering applications for regenerative medicine in humans. Several iTSC types have been identified, including iTS-L, iTS-P, and iTS-D, obtained by reprogramming hepatocytes, pancreatic cells, and deciduous tooth-derived dental pulp cells, respectively. This review provides a brief overview of iPSCs and discusses recent advances in the establishment of iTSCs and their possible applications in regenerative medicine.
  • 986
  • 11 Oct 2021
Topic Review
DDS Based on Polysaccharides
Polysaccharides are polymeric carbohydrates composed of repeating monomeric units of monosaccharides that are covalently linked to each other through glucosidic linkage. Polysaccharides are biocompatible, biodegradable biopolymers, and the presence of various functional groups, such as hydroxyl, carboxyl, and amino groups, allow their easy chemical modification in order to increase their intrinsic properties (solubility, chemical stability, etc.). Due to these improved properties, polysaccharides are largely used as biomaterials in food, biomedical, pharmaceutical, cosmetic industry, and also as micellar drug-loaded systems. 
  • 985
  • 12 Apr 2021
Topic Review
4D Printing Technology
4D printing (4DP) is an evolution of 3DP where additive manufacturing printing techniques are employed. In other words, adapting 3DP processes for 4DP of shape memory polymers (SMPs) or smart materials requires minor adjustments. In order to produce the desired shape-changing materials as per estimation or for optimal application, an air circulation system may be incorporated into 3DP’s traditional fused deposition method (FDM) technology. This would cool the SMP below its Tg and, after these small alterations, previous 3DP methods such as stereolithography apparatus (SLA), digital laser writing and inkjet printing can also be employed.
  • 985
  • 05 Jan 2023
Topic Review
Non-Alkaloid Cholinesterase Inhibitory Compounds
The classes of cholinesterase inhibitors discussed here are mainly terpenoids, phenolic compounds, and coumarins, and some of these compounds have shown high potency. In order to consider which classes are most suitable, based on the benefits and drawbacks, certain structural features of each class will be of great importance. Using chalcones as an example, it is believed that besides economical and cost-effective production, small molecular size and flexibility for modifications to improve lipophilicity necessary for blood-brain barrier permeability are important to consider for a preferred potential therapeutic candidate for AD.
  • 984
  • 29 Sep 2021
Topic Review
Fexinidazole: All-Oral Therapy for Human African Trypanosomiasis
Human African trypanosomiasis (HAT or ‘sleeping sickness’) is a neglected tropical disease. If untreated, it is always fatal and leads to death. A few treatments are available for HAT, but most of them require a skilled professional, which increases the financial burden on the patient. Recently, fexinidazole (FEX) has been approved by the European Medicine Agency (EMA) and the United States Food and Drug Administration (USFDA) as the first all-oral therapy for the treatment of stage-1 (hemolymphatic) as well as stage-2 (meningoencephalitic) of HAT. Before the FEX approval, there were separate treatments for stage-1 and stage-2 of HAT. 
  • 982
  • 25 Jan 2022
Topic Review
Traditional Cancer Healing with Herbs and Mushrooms
Traditional herbal medicine (THM) is a “core” from which modern medicine has evolved over time. Besides this, one third of people worldwide have no access to modern medicine and rely only on traditional medicine. To date, drugs of plant origin, or their derivates (paclitaxel, vinblastine, vincristine, vinorelbine, etoposide, camptothecin, topotecan, irinotecan, and omacetaxine), are very important in the therapy of malignancies and they are included in most chemotherapeutic regimes. 
  • 982
  • 28 Jul 2022
Topic Review
Natural Photoprotectants From Sea
The thinning of the ozone layer due to increased atmospheric pollution has exacerbated the negative effects of excessive exposure to solar ultraviolet radiation (UVR), and skin cancer has become a major public health concern. In order to prevent skin damage, public health advice mainly focuses on the use of sunscreens, along with wearing protective clothing and avoiding sun exposure during peak hours. Sunscreens present on the market are topical formulations that contain a number of different synthetic, organic, and inorganic UVR filters with different absorbance profiles, which, when combined, provide broad UVR spectrum protection. However, increased evidence suggests that some of these compounds cause subtle damage to marine ecosystems. One alternative may be the use of natural products that are produced in a wide range of marine species and are mainly thought to act as a defense against UVR-mediated damage.
  • 981
  • 28 Jul 2021
Topic Review
Ruthenium Complexes
Ruthenium(Ru)-complexes go beyond the limitations of Platinum(Pt)-based drugs, notably oxaliplatin, and exhibit higher potency while offering less toxicity in colorectal cancer (CRC) treatment. Therefore, Ru-complexes can be a promising alternative to oxaliplatin in CRC treatment. 
  • 981
  • 08 Sep 2021
Topic Review
Classification of Allosteric G-Protein-Coupled Receptors Regulators
Allosteric regulation is critical for the functioning of G-protein-coupled receptors (GPCRs) and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions, various biomolecules (lipids, amino acids, polypeptides, hormonal agents, etc.), and the peptide components of GPCR signaling. According to the ability to influence the basal and orthosteric/allosteric agonist-stimulated activity, the ligands of GPCR allosteric sites can be divided into the positive (PAM), negative (NAM), and silent (SAM) allosteric modulators, the allosteric full agonists, inverse agonists and neutral antagonists, as well as the allosteric regulators with the combined activity (ago-PAM, ago-NAM). 
  • 981
  • 19 Apr 2023
Topic Review
Botryllus schlosseri
Botryllus schlosseri, a colonial tunicate, which is the nearest invertebrate group to the vertebrates, is devoid of T- and B-cell-based adaptive immunity. It has unique characteristics that make it a valuable model system for studying innate immunity mechanisms: (i) a natural allogeneic transplantation phenomenon that results in either fusion or rejection; (ii) whole animal regeneration and noninflammatory resorption on a weekly basis; (iii) allogeneic resorption which is comparable to human chronic rejection. Recent studies in B. schlosseri have led to the recognition of a molecular and cellular framework underlying the innate immunity loss of tolerance to allogeneic tissues. Additionally, B. schlosseri was developed as a model for studying hematopoietic stem cell (HSC) transplantation, and it provides further insights into the similarities between the HSC niches of human and B. schlosseri. The entry is from Botryllus schlosseri as a Unique Colonial Chordate Model for the Study and Modulation of Innate Immune Activity. August 2021Marine Drugs 19(8):454. DOI: 10.3390/md19080454
  • 978
  • 30 Aug 2021
Topic Review
Critically Ill Patients Antimicrobial Dosing
In recent years, the knowledge of pharmacokinetics and pharmacodynamics, drug dosing, therapeutic drug monitoring, and antimicrobial resistance in the critically ill patients has greatly improved, fostering strategies to optimize therapeutic efficacy and to reduce toxicity and adverse events. Nonetheless, delivering adequate and appropriate antimicrobial therapy is still a challenge, since pathogen resistance continues to rise, and new therapeutic agents remain scarce. 
  • 978
  • 13 Jul 2021
Topic Review
Ivabradine Effects on Cardiac Function
Cardiac remodeling can cause ventricular dysfunction and progress to heart failure, a cardiovascular disease that claims many lives globally. Ivabradine, a funny channel (If) inhibitor, is used in patients with chronic heart failure as an adjunct to other heart failure medications.
  • 977
  • 10 Feb 2023
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