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Topic Review
Thiazole-Based Peptides
Peptides are distinctive biomacromolecules that demonstrate potential cytotoxicity and diversified bioactivities against a variety of microorganisms including bacteria, mycobacteria, and fungi via their unique mechanisms of action. Among broad-ranging pharmacologically active peptides, natural marine-originated thiazole-based oligopeptides possess peculiar structural features along with a wide spectrum of exceptional and potent bioproperties. Because of their complex nature and size divergence, thiazole-based peptides (TBPs) bestow a pivotal chemical platform in drug discovery processes to generate competent scaffolds for regulating allosteric binding sites and peptide–peptide interactions. The present study dissertates on the natural reservoirs and exclusive structural components of marine-originated TBPs, with a special focus on their most pertinent pharmacological profiles, which may impart vital resources for the development of novel peptide-based therapeutic agents.
  • 741
  • 22 Sep 2020
Topic Review
Nonribosomal Peptide and Polyketide Against Human Pathogens
Antibiotics are majorly important molecules for human health. Following the golden age of antibiotic discovery, a period of decline ensued, characterised by the rediscovery of the same molecules. At the same time, new culture techniques and high-throughput sequencing enabled the discovery of new microorganisms that represent a potential source of interesting new antimicrobial substances to explore. 
  • 741
  • 15 Nov 2021
Topic Review
Micro- and Nanosized Carriers for Nose-to-Brain Drug Delivery
The intranasal route of drug administration offers numerous advantages, such as bypassing the intestine, avoiding first-pass metabolism, and reducing systemic side effects. Moreover, it circumvents the BBB, providing direct entrance to the brain through the olfactory and trigeminal nerve pathways.  Micro- and nanotechnological approaches were widely used to overcome these limitations and enhance the availability of drugs in the brain tissue. Micro- and nanoparticulate carriers are composed of natural or synthetic materials that interact with biological structures at the molecular level and lead the treatment of NDs into a new direction. They may induce interaction between target sites, thus minimizing the side effects.
  • 741
  • 22 Aug 2022
Topic Review
Pomegranate Juice for CYP3A4- and CYP2C9-Mediated Drugs Metabolism
The Punica granatum L. (pomegranate) fruit juice contains large amounts of polyphenols, mainly tannins such as ellagitannin, punicalagin, and punicalin, and flavonoids such as anthocyanins, flavan-3-ols, and flavonols. These constituents have high antioxidant, anti-inflammatory, anti-diabetic, anti-obesity, and anticancer activities. Because of these activities, many patients may consume pomegranate juice (PJ) with or without their doctor’s knowledge. This may raise any significant medication errors or benefits because of food-drug interactions that modulate the drug’s pharmacokinetics or pharmacodynamics. 
  • 741
  • 18 May 2023
Topic Review
Exosome-Based Drug Delivery in Lupus
Exosomes are lipid-bilayer-enclosed extracellular vesicles released by many cell types in both normal and pathological conditions, and which transport nucleic acids, lipids and proteins between cells. Due to their suitable proprieties, as well as their known therapeutic effects, exosome-based nanocarriers have a bright future as next-generation drug delivery vehicles.
  • 740
  • 18 Mar 2021
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.
  • 737
  • 13 Apr 2022
Topic Review
Hydrodynamic Delivery
The principle of hydrodynamic delivery was initially used to develop a method for delivering plasmids into mouse hepatocytes through tail vein injection and has since been expanded for use in delivering various biologically active materials to cells in different organs of several animal species. 
  • 732
  • 18 Apr 2023
Topic Review
Dinoflagellate Phycotoxins
Dinoflagellates are single-celled eukaryotes constitute an important group of phytoplanktons, characterized by two dissimilar flagella and distinctive features of both plants and animals.
  • 730
  • 30 Dec 2020
Topic Review
Adiponectin System (Rescue Hormone)
The adipose tissue, regardless of its role in generating and storing energy, acts as a key player as an endocrine tissue, producing a wide scale of cytokines/hormones called adipokines. Adipokines such as leptin, resistin, visfatin and osteopontin own pro-inflammatory effects on the cardiovascular system in some cases. In contrast, some adipokines have cardioprotective and anti-inflammatory impacts including adiponectin, omentin, and apelin.
  • 730
  • 12 Jul 2022
Topic Review
Lipid Nanoparticulate Drug Delivery Systems and Skin Disorders
Lipid nanoparticles (LN) are recognized as promising drug delivery systems (DDS) in treating skin disorders. Solid lipid nanoparticles (SLN) together with nanostructured lipid carriers (NLC) exhibit excellent tolerability as these are produced from physiological and biodegradable lipids. Moreover, LN applied to the skin can improve stability, drug targeting, occlusion, penetration enhancement, and increased skin hydration compared with other drug nanocarriers. Furthermore, the features of LN can be enhanced by inclusion in suitable bases such as creams, ointments, gels (i.e., hydrogel, emulgel, bigel), lotions, etc. 
  • 728
  • 16 Nov 2021
Topic Review
Fenretinide in Cancer and Neurological Disease
Cancer and neurodegeneration share leadership as causes of morbidity and death worldwide. They can be thought as disease mechanisms at opposite ends: while in neurodegeneration, induction of inflammatory genes and suppression of cell-cycle genes are the prominent signals; the opposite happens in cancer. Fenretinide (all-trans-N-(4-hydroxyphenyl) retinamide, 4-HPR) is a synthetic derivative of all-trans-retinoic acid initially proposed in anticancer therapy for its antitumor effects combined with limited toxicity. It is also studied in many other diseases for its ability to influence several biological pathways and provide a broad spectrum of pharmacological effects.
  • 728
  • 18 Jul 2022
Topic Review
Biopolymer Based Prodrugs as Potential Antineoplastic Therapy
Cancer represents a major public health issue, a substantial economic issue, and a burden for society. Limited by numerous disadvantages, conventional chemotherapy is being replaced by new strategies targeting tumor cells. In this context, therapies based on biopolymer prodrug systems represent a promising alternative for improving the pharmacokinetic and pharmacologic properties of drugs and reducing their toxicity. The polymer-directed enzyme prodrug therapy is based on tumor cell targeting and release of the drug using polymer–drug and polymer–enzyme conjugates. In addition, current trends are oriented towards natural sources. They are biocompatible, biodegradable, and represent a valuable and renewable source. Drug–polymer conjugates based on natural polymers such as chitosan (CTS), hyaluronic acid (HA), dextran (DEX), pullulan (PL), silk fibroin (SF), centyrins (CTR), heparin (HEP), and polysaccharides from Auricularia auricula (AAP) are presented. 
  • 728
  • 19 Sep 2022
Topic Review
Grimelysin and Protealysin
The entry reviews the discovery, properties, and functional activities of new bacterial enzymes, proteases grimelysin (ECP 32) of Serratia grimesii and protealysin of Serratia proteamaculans, characterized by both a highly specific “actinase” activity and their ability to stimulate bacterial invasion. Grimelysin cleaves the only one polypeptide bond Gly42-Val43 in actin. This bond is not cleaved by any other proteases and leads to a reversible loss of actin polymerization. Similar properties were characteristic for another bacterial protease, protealysin. These properties made grimelysin and protealysin a unique tool to study the functional properties of actin. Furthermore, bacteria Serratia spp. producing grimelysin/protealysin invade eukaryotic cells, and the recombinant Escherichia coli expressing the grimelysin or protealysins gene become invasive. Being an intracellular enzyme, grimelysin/protealysin can be delivered by bacteria to eukaryotic cells. These data indicate that the protease is a virulence factor, and actin can be a target for the protease upon its translocation into the host cell.
  • 726
  • 27 Oct 2020
Topic Review
Three-Dimensional Spheroids in Cancer Research
Three-dimensional (3D) cultures of cancer cells that better recapitulate in vivo cell environments emerged as scientifically accurate and low cost cancer models for preclinical screening and testing of new drug candidates before moving to expensive and time-consuming animal models.
  • 724
  • 09 Dec 2020
Topic Review
Sustained Antiviral Ocular Drug Delivery
The eyes are the window to the world and the key to communication, but they are vulnerable to multitudes of ailments. More serious than is thought, corneal infection by herpes simplex viruses (HSVs) is a prevalent yet silent cause of blindness in both the paediatric and adult population, especially if immunodeficient. Globally, there are 1.5 million new cases and forty thousand visual impairment cases reported yearly. The Herpetic Eye Disease Study recommends topical antiviral as the front-line therapy for HSV keratitis. Ironically, topical eye solutions undergo rapid nasolacrimal clearance, which necessitates oral drugs but there is a catch of systemic toxicity. The hurdle of antiviral penetration to reach an effective concentration is further complicated by drugs’ poor permeability and complex layers of ocular barriers.
  • 724
  • 02 Feb 2021
Topic Review Peer Reviewed
Biofunctional Peptide FNIII14: Therapeutic Potential
Biofunctional peptide FNIII14, which is derived from the 14th fibronectin (FN) type III-like (FN-III) repeat of FN molecule, is capable of inhibiting cell adhesion to the extracellular matrix (ECM). This functional site is usually buried within the molecular structure of FN, but can be exposed by conformational changes and proteolytic cleavage. Peptide FNIII14 can induce a conformational change in β1-integrin from the active to the inactive form, causing functional inactivation. Based on this anti-adhesive activity, peptide FNIII14 exhibits therapeutic potential for several diseases such as metabolic diseases, organ fibrosis, and malignant tumors. Peptide FNIII14 blocks integrin-mediated signaling by a mechanism entirely distinct from that of conventional antagonisitic peptides, including Arg-Gly-Asp peptides that competitively inhibit the ECM binding of integrin. 
  • 724
  • 13 Apr 2022
Topic Review
Blood–Brain Barrier
The blood–brain barrier (BBB) is a natural obstacle for drug delivery into the human brain, hindering treatment of central nervous system (CNS) disorders such as acute ischemic stroke, brain tumors, and human immunodeficiency virus (HIV)-1-associated neurocognitive disorders.
  • 724
  • 27 Apr 2021
Topic Review
Cryptocyanine Dye, NK-4
NK-4 plays a key role in the treatment of various diseases, such as in hay fever to expect anti-allergic effects, in bacterial infections and gum abscesses to expect anti-inflammatory effects, in scratches, cuts, and mouth sores from bites inside the mouth for enhanced wound healing, in herpes simplex virus (HSV)-1 infections for antiviral effects, and in peripheral nerve disease that causes tingling pain and numbness in hands and feet, while NK-4 is used also to expect antioxidative and neuroprotective effects.
  • 724
  • 08 Mar 2023
Topic Review
Insights into the Pharmacological Effects of Flavonoids
Flavonoids are widely occurring secondary metabolites of plants. Currently, there is a trend of article numbers increasing, which focuses on the computer modeling of flavonoid interactions with biological targets. Such studies help to accumulatethe data on lead compounds that can find medicinal implementation, including COVID-19. Flavanonol taxifolin demonstrated wound-healing activity. Luteolin, apigenin, and wogonin, which can be classified as flavones, show induced neutrophil apoptosis and have potential as neutrophil apoptosis-inducing anti-inflammatory, proresolution agents.
  • 723
  • 10 Jun 2022
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.
  • 721
  • 09 Sep 2021
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