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Topic Review
Anti-Leishmania Drug Delivery Systems
Two series of new hybrid γ/γ-peptides, γ-CC and γ-CT, formed by (1S,2R)-3-amino-2,2-dimethylcyclobutane-1-carboxylic acid joined in alternation to a Nα-functionalized cis- or trans-γ-amino-L-proline derivative, respectively, have been synthesized and evaluated as cell penetrating peptides (CPP) and as selective vectors for anti-Leishmania drug delivery systems (DDS). They lacked cytotoxicity on the tumoral human cell line HeLa with a moderate cell-uptake on these cells. In contrast, both γ-CC and γ-CT tetradecamers were microbicidal on the protozoan parasite Leishmania beyond 25 μM, with significant intracellular accumulation. They were conjugated to fluorescent doxorubicin (Dox) as a standard drug showing toxicity beyond 1 μM, while free Dox was not toxic. Intracellular accumulation was 2.5 higher than with Dox-TAT conjugate (TAT = transactivator of transcription, taken as a standard CPP). The conformational structure of the conjugates was approached both by circular dichroism spectroscopy and molecular dynamics simulations. Altogether, computational calculations predict that the drug-γ-peptide conjugates adopt conformations that bury the Dox moiety into a cavity of the folded peptide, while the positively charged guanidinium groups face the solvent. The favorable charge/hydrophobicity balance in these CPP improves the solubility of Dox in aqueous media, as well as translocation across cell membranes, making them promising candidates for DDS.
  • 1.0K
  • 20 Oct 2020
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.
  • 1.0K
  • 02 Aug 2023
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). 
  • 1.0K
  • 19 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. 
  • 1.0K
  • 03 Nov 2023
Topic Review
Autophagy in Nanomaterial Toxicity
Nanotechnology has rapidly promoted the development of a new generation of industrial and commercial products; however, it has also raised some concerns about human health and safety. To evaluate the toxicity of the great diversity of nanomaterials (NMs) in the traditional manner, a tremendous number of safety assessments and a very large number of animals would be required. For this reason, it is necessary to consider the use of alternative testing strategies or methods that reduce, refine, or replace (3Rs) the use of animals for assessing the toxicity of NMs. Autophagy is considered an early indicator of NM interactions with cells and has been recently recognized as an important form of cell death in nanoparticle-induced toxicity. Impairment of autophagy is related to the accelerated pathogenesis of diseases. By using mechanism-based high-throughput screening in vitro, we can predict the NMs that may lead to the generation of disease outcomes in vivo. Thus, a tiered testing strategy is suggested that includes a set of standardized assays in relevant human cell lines followed by critical validation studies carried out in animals or whole organism models such as C. elegans (Caenorhabditis elegans), zebrafish (Danio rerio), and Drosophila (Drosophila melanogaster)for improved screening of NM safety. A thorough understanding of the mechanisms by which NMs perturb biological systems, including autophagy induction, is critical for a more comprehensive elucidation of nanotoxicity. A more profound understanding of toxicity mechanisms will also facilitate the development of prevention and intervention policies against adverse outcomes induced by NMs. The development of a tiered testing strategy for NM hazard assessment not only promotes a more widespread adoption of non-rodent or 3R principles but also makes nanotoxicology testing more ethical, relevant, and cost- and time-efficient.
  • 1.0K
  • 28 Oct 2020
Topic Review
Vitamin K Antagonists
The efficacy and safety of vitamin K antagonists (VKAs) as oral anticoagulants (OACs) depend on the quality of anticoagulation control, as reflected by the mean time in therapeutic range (TTR). 
  • 1.0K
  • 12 Apr 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.
  • 996
  • 11 Oct 2021
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.
  • 996
  • 29 Sep 2021
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.
  • 996
  • 11 Nov 2021
Topic Review
Pharmacological Activities of Betulin
Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways.
  • 996
  • 25 Jul 2023
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.
  • 995
  • 16 Dec 2020
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.
  • 995
  • 05 Jan 2023
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. 
  • 994
  • 12 Apr 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. 
  • 994
  • 25 Jan 2022
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.
  • 993
  • 11 Oct 2021
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.
  • 992
  • 09 Sep 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. 
  • 992
  • 13 Jul 2021
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.
  • 990
  • 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. 
  • 990
  • 08 Sep 2021
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
  • 989
  • 30 Aug 2021
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