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Topic Review
Immunoproteasome
Proteasome inhibition is a promising strategy for the treatment of multiple myeloma; unfortunately, this disease is often associated with an increasing chemoresistance. One novel approach may be to target the immunoproteasome, a proteasomal isoform mainly present in cells of hematopoietic origin. We investigated the activity of a panel of amides against immunoproteasome core particles as potential agents for the treatment of multiple myeloma (MM). Amide 6 showed an ideal profile since it was able to inhibit both the chymotrypsin-like activities of the immunoproteasome with Ki values of 4.90 µM and 4.39 µM for β1i and β5i, respectively, coupled with an EC50 =17.8 µM against MM.1R cells. Compound 6 inhibited also ubiquitinated protein degradation and was able to act on different phases of MM cell cycle reducing the levels of cyclin A/CDK1, cyclin B/CDK1 and cyclin D/CDK4/6 complexes, which turns in cell cycle arrest.
  • 1.0K
  • 03 Nov 2020
Topic Review
Nuclear Factor Erythroid 2-Related Factor 2
Being a controller of cytoprotective actions, inflammation, and mitochondrial function through participating in the regulation of multiple genes in response to stress-inducing endogenous or exogenous stressors, the transcription factor Nuclear Factor Erythroid 2-Related Factor 2 (NRF2) is considered the main cellular defense mechanism to maintain redox balance at cellular and tissue level. While a transient activation of NRF2 protects normal cells under oxidative stress, the hyperactivation of NRF2 in cancer cells may help them to survive and to adapt under oxidative stress. This can be detrimental and related to cancer progression and chemotherapy resistance. Therefore, inhibition of NRF2 activity may be an effective approach for sensitizing cancer cells to anticancer therapy.
  • 1.0K
  • 14 Jun 2023
Topic Review Peer Reviewed
Photobiomodulation for Taste Alteration
Photobiomodulation (PBM) therapy employs light at red and near-infrared wavelengths to modulate biological activity. The therapeutic effect of PBM for the treatment or management of several diseases and injuries has gained significant popularity among researchers and clinicians, especially for the management of oral complications of cancer therapy. This entry focuses on the current evidence on the use of PBM for the management of a frequent oral complication due to cancer therapy—taste alteration.
  • 1.0K
  • 13 Apr 2022
Topic Review
Animal Lectins
Animal lectins are proteins with carbohydrate recognition activity. Galectins, the β-galactoside binding lectins, are expressed in various cells and have been reported to regulate several immunological and physiological responses. Recently, some galectins have been reported to regulate some viral infections, including influenza A virus (IAV); however, the mechanism is still not fully understood.
  • 1.0K
  • 31 May 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.
  • 1.0K
  • 25 Jul 2023
Topic Review
Sphingosine-1-Phosphate and Platelets in Diseases
Sphingosine-1-phosphate (S1P) is a versatile signaling lipid involved in the regulation of numerous cellular processes. S1P regulates cellular proliferation, migration, and apoptosis as well as the function of immune cells. S1P is generated from sphingosine (Sph), which derives from the ceramide metabolism. In particular, high concentrations of S1P are present in the blood. This originates mainly from erythrocytes, endothelial cells (ECs), and platelets. While erythrocytes function as a storage pool for circulating S1P, platelets can rapidly generate S1P de novo, store it in large quantities, and release it when the platelet is activated. Platelets can thus provide S1P in a short time when needed or in the case of an injury with subsequent platelet activation and thereby regulate local cellular responses. In addition, platelet-dependently generated and released S1P may also influence long-term immune cell functions in various disease processes, such as inflammation-driven vascular diseases. New pharmacological approaches that target the auto- or paracrine effects of S1P may be therapeutically helpful in the future for pathological processes involving S1P.
  • 1.0K
  • 15 Sep 2022
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.
  • 1.0K
  • 29 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.
  • 1.0K
  • 16 Dec 2020
Topic Review
Nanotheranostics for Atherosclerosis
Atherosclerosis refers to the pathophysiological conditions where the medium and large arteries are significantly affected due to spatial deposition of various materials such as lipoproteins (particularly cholesterol), immune cells (circulating monocytes), proinflammatory factors (i.e., macrophages and T-cells), degraded extracellular matrix components and necrotic products. Atherosclerosis is considered to be the primary cause of chronic CVDs, including coronary heart disease, cerebrovascular disease, and peripheral arterial disease. Atherosclerosis is characterized by a series of physiological events, including endothelial dysfunction, inflammatory responses, cell proliferation, lipoprotein deposition, vascular remodeling, and finally, plaque formation.
  • 1.0K
  • 15 Apr 2021
Topic Review
Biomedical Applications of mRNA Using Nanomedicine
The development and commercialization of mRNA COVID-19 vaccines have pivoted the way towards future applications of mRNA medicines by finally finding a solution to the problem of delivery. Despite concerns from detractors about a lack of applications for nanotechnology, nanomedicine has now demonstrated that it is a translational, relevant and much-needed approach to engineer new genetic drugs. Thus, it is now clear that the full potential of mRNA therapeutics, along with its advantages could not be envisioned without nanomedicine.
  • 1.0K
  • 07 Mar 2022
Topic Review
Risk of Adverse Drug Reactions in Elderly Population
The European Medicine Agency (EMA) has defined Adverse Drug Reactions (ADRs) as “a noxious and unintended response to a medicine”, not including poisoning, accidental, or intentional overdoses. The ADR occurrence differs based on the approach adopted for defining and detecting them, the characteristics of the population under study, and the research setting. ADRs have a significant impact on morbidity and mortality, particularly among older adults, and represent a financial burden for health services.
  • 1.0K
  • 09 Nov 2023
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.
  • 1.0K
  • 10 Feb 2023
Topic Review
Physicochemical Characterization of Aluminum Adjuvants
Aluminum-based adjuvants will continue to be a key component of currently approved and next generation vaccines. Their large adsorptive capacity allows the combination with other immunostimulatory molecules to create a toolbox of adjuvants for selective vaccine applications. The widespread use of aluminum adjuvants is due to their excellent safety profile, which has been established through the use of hundreds of millions of doses in humans over many years, low cost, and extensive experience with licensure through regulatory agencies.
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  • 25 Jul 2023
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
Nefroprotective Potential of Amazonian Plant Species
There are several Amazonian plant species with potential pharmacological validation for the treatment of acute kidney injury, a condition in which the kidneys are unable to adequately filter the blood, resulting in the accumulation of toxins and waste in the body. 
  • 1.0K
  • 14 Sep 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
American Ginseng Berry and its Mental Health Applications
Despite the popularity of the ginseng (Panax) root in health research and on the market, the ginseng berry’s potential remains relatively unexplored. Implementing ginseng berry cultivations and designing berry-derived products could improve the accessibility to mental health-promoting nutraceuticals.
  • 1.0K
  • 30 Jun 2022
Topic Review
Nanotheranostic Platforms
Globally, cancer is one of the deadliest diseases, needing a meticulous diagnosis and targeted treatment plan to achieve an initial prognosis, followed by precision and optimization in treatment. Nonselective targeting, difficulty in accurately monitoring treatment end-results, serious drug side-effects, and severity of disease resulting in metastasis are the key flaws of traditional techniques. Nanotechnology and nanoparticles possess special features to completely transform the field of diagnosis and treatment of cancer.
  • 1.0K
  • 16 Aug 2023
Topic Review
Neurological Diseases and Their Biomarkers
Neurodegenerative diseases (NDDs) are disorders that affect both the central and peripheral nervous systems. To name a few causes, NDDs can be caused by ischemia, oxidative and endoplasmic reticulum (ER) cell stress, inflammation, abnormal protein deposition in neural tissue, autoimmune-mediated neuron loss, and viral or prion infections.
  • 1.0K
  • 07 Jun 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.
  • 1.0K
  • 11 Oct 2021
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