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Topic Review
Antibiotic Hybrids
An emerging strategy in the fight against antimicrobial resistance is the development of antibiotic hybrids. The term “hybrid” suggests a two-component molecule with biological activity that retains the activity of the individual components after hybridization, acting synergistically. For example, hybrid drugs that incorporate two active compounds into a single molecule could be used to expand the biological activity and prevent the development of bacterial resistance.
  • 1.1K
  • 22 Sep 2022
Topic Review
Lipid-Based Nanoparticles as a Versatile Drug Delivery System
Liposomes, nanoemulsions, solid lipid nanoparticles, nanostructured lipid nanocarriers, and lipid–polymer hybrid nanoparticles are developed for cancer treatment which is well confirmed and documented. cancer nanotechnology that overcomes the drawbacks of conventional drug delivery systems starting from small-scale barricades such as intracellular trafficking and site-specific targeting to large-scale barriers such as biodistribution.
  • 1.1K
  • 27 Sep 2022
Topic Review
TIGIT
TIGIT is a transmembrane glycoprotein comprising one immunoglobulin variable (IgV) domain, a type I transmembrane domain, and a cytoplasmic tail with an immunoreceptor tyrosine-based inhibitory motif (ITIM) and immunoglobulin tyrosine tail (ITT)-like motif.
  • 1.1K
  • 08 Apr 2021
Topic Review
The Applications of Phlorotannins
Phlorotannins are a type of natural active substance extracted from brown algae, which belong to a type of important plant polyphenol. Phloroglucinol is the basic unit in its structure. Phlorotannins have a wide range of biological activities, such as antioxidant, antibacterial, antiviral, anti-tumor, anti-hypertensive, hypoglycemic, whitening, anti-allergic and anti-inflammatory, etc. Phlorotannins are mainly used in the fields of medicine, food and cosmetics. 
  • 1.0K
  • 12 Dec 2022
Topic Review
Delpazolid for Tuberculosis Treatment
A novel oxazolidinone with cyclic amidrazone, delpazolid (LCB01-0371), was synthesized by LegoChem BioSciences, Inc. (Daejeon, Korea). Delpazolid can improve the minimum bactericidal concentration of Mycobacterium tuberculosis H37Rv and significantly reduce resistance rates,especially of multi-drug-resistant tuberculosis (MDR-TB) isolates, compared with linezolid. Therefore, delpazolid can be used to treat MDR-TB. The safety, tolerability, and pharmacokinetics of delpazolid have been evaluated in a phase 1 clinical trial, which revealed that it does not cause adverse events such as myelosuppression even after three weeks of repeated dosing. 
  • 1.0K
  • 29 Oct 2020
Topic Review
Thymus algeriensis Boiss. and Reut.
The word Thymus comes from the Greek “thyo”, which means “offering” (to be burnt) and “perfume” because of the pleasant smell that the plant gives off naturally when burnt. T. algeriensis Boiss. and Reut. are classified in section Hyphodromi (A. Kerner) Haläcsy and subsection Subbracteati (Klokov) Jalas. It belongs to the order Lamiale, subfamily Nepetoideae, and tribe Menthae.
  • 1.0K
  • 30 Dec 2022
Topic Review
Marine Algae-Derived Bioactive Compounds
Marine algae are rich in bioactive nutraceuticals (e.g., carbohydrates, proteins, minerals, fatty acids, antioxidants, and pigments). Biotic (e.g., plants, microorganisms) and abiotic factors (e.g., temperature, pH, salinity, light intensity) contribute to the production of primary and secondary metabolites by algae. Easy, profitable, and sustainable recovery methods include novel solid-liquid and liquid-liquid extraction techniques (e.g., supercritical, high pressure, microwave, ultrasound, enzymatic). The spectacular findings of algal-mediated synthesis of nanotheranostics has attracted further interest because of the availability of microalgae-based natural bioactive therapeutic compounds and the cost-effective commercialization of stable microalgal drugs. 
  • 1.0K
  • 07 Sep 2021
Topic Review
Liposomal Delivery Systems
The versatility of liposomal carriers does not just simply rely on their capability to encapsulate various types of therapeutic substances, but also on the large array of components used for constructing liposome-based nanoformulations that allow for a straightforward control over targeting and the release of the encapsulated contents. This leads to a wide array of design strategies which can be easily adapted to any desired theraupetic effect, rendering liposomes one of the most promising systems for drug delivery. 
  • 1.0K
  • 20 Jan 2021
Topic Review
β-Lactamase Inhibitors
The inhibitors of β-lactamases (BLI) have gained a prominent role in the safeguard of beta-lactams. In the last years, new β-lactam–BLI combinations have been registered or are still under clinical evaluation, demonstrating their effectiveness to treat complicated infections. It is also noteworthy that the pharmacokinetics of BLIs partly matches that of β-lactams companions, meaning that some clinical situations, as well as renal impairment and renal replacement therapies, may alter the disposition of both drugs. Common pharmacokinetic characteristics, linear pharmacokinetics across a wide range of doses, and known pharmacokinetic/pharmacodynamic parameters may guide modifications of dosing regimens for both β-lactams and BLIs. However, comorbidities (i.e., burns, diabetes, cancer) and severe changes in individual pathological conditions (i.e., acute renal impairment, sepsis) could make dose adaptation difficult, because the impact of those factors on BLI pharmacokinetics is partly known. Therapeutic drug monitoring protocols may overcome those issues and offer strategies to personalize drug doses in the intensive care setting. Further prospective clinical trials are warranted to improve the use of BLIs and their β-lactam companions in severe and complicated infections. 
  • 1.0K
  • 11 Jul 2021
Topic Review
Bacterial Virulence Factors
There are several levels to influence the expression of eukaryotic genes. A first level of interference is changing of the DNA’s structure on the chromatin level. Epigenetic modulation enables remodelling of the chromatin to transfer heterochromatin into euchromatin allowing transcription or vice versa. In addition, the affinity of promotors and other regulatory DNA sequences for RNA polymerases and transcription factors (TFs) can be influenced by cytosine or adenine methylation. Only a minor portion (fewer than 2%) of genes is transcribed into mRNAs, instead the majority is transferred into so called non-coding RNAs (ncRNAs). Certain long ncRNAs (lncRNAs) are also involved in epigenetic regulations. Epigenetic mechanisms are used for manipulation of gene expression in the course of several cellular processes. Here, we give an overview on the epigenetic control of gene expression by bacterial virulence factors during host cell infection.
  • 1.0K
  • 27 Oct 2020
Topic Review
Oximes
Oximes have been studied for decades because of their significant roles as acetylcholinesterase reactivators. Over the last twenty years, a large number of oximes have been reported with useful pharmaceutical properties, including compounds with antibacterial, anticancer, anti-arthritis, and anti-stroke activities. Many oximes are kinase inhibitors and have been shown to inhibit over 40 different kinases, including AMP-activated protein kinase (AMPK), phosphatidylinositol 3-kinase (PI3K), cyclin-dependent kinase (CDK), serine/threonine kinases glycogen synthase kinase 3 α/β (GSK-3α/β), Aurora A, B-Raf, Chk1, death-associated protein-kinase-related 2 (DRAK2), phosphorylase kinase (PhK), serum and glucocorticoid-regulated kinase (SGK), Janus tyrosine kinase (JAK), and multiple receptor and non-receptor tyrosine kinases. Some oximes are inhibitors of lipoxygenase 5, human neutrophil elastase, and proteinase 3. The oxime group contains two H-bond acceptors (nitrogen and oxygen atoms) and one H-bond donor (OH group), versus only one H-bond acceptor present in carbonyl groups. This feature, together with the high polarity of oxime groups, may lead to a significantly different mode of interaction with receptor binding sites compared to corresponding carbonyl compounds, despite small changes in the total size and shape of the compound. In addition, oximes can generate nitric oxide.
  • 1.0K
  • 03 Jun 2021
Topic Review
Mechanisms of Resistance to Gemcitabine
Gemcitabine is still the standard-of-care chemotherapeutic drug for pancreatic ductal adenocarcinoma (PDAC). However, the response rate is quite low. There are multiple mechanisms and participants in gemcitabine resistance.
  • 1.0K
  • 01 Jun 2022
Topic Review
HIV-1
The HIV-1 integrase enzyme (IN) plays a critical role in the viral life cycle by integrating the reverse-transcribed viral DNA into the host chromosome. This function of IN has been well studied, and the knowledge gained has informed the design of small molecule inhibitors that now form key components of antiretroviral therapy regimens. Recent discoveries unveiled that IN has an under-studied yet equally vital second function in HIV-1 replication. This involves IN binding to the viral RNA genome in virions, which is necessary for proper virion maturation and morphogenesis. Herein we describe these two functions of IN within the context of the HIV-1 life cycle, how IN binding to the viral genome is coordinated by the major structural protein, Gag, and discuss the value of targeting the second role of IN in virion morphogenesis.
  • 1.0K
  • 17 Sep 2020
Topic Review
Lewy Body Dementia Mice Model
Lewy bodies are pathological characteristics of Lewy body dementia (LBD) and are composed of α-synuclein (α-Syn), which is mostly degraded via the ubiquitin–proteasome system. More importantly, 26S proteasomal activity decreases in the brain of LBD patients. 
  • 1.0K
  • 22 Sep 2021
Topic Review
Therapeutic Actions of Anthocyanins in Chronic Diseases
Anthocyanins are secondary metabolites and distributed in flowers, fruits and vegetables. They provide various colours such as red, pink, blue and purple. To date, more than 700 anthocyanins have been identified in nature. These anthocyanins have been associated with many health benefits through different mechanisms. Some of the therapeutic potentials of anthocyanins and their mechanisms of action are highlighted.
  • 1.0K
  • 18 Sep 2022
Topic Review
Plant-Anticancer Compounds in Cancer Treatment
Nowadays, cancer is one of the deadliest diseases in the world, which has been estimated to cause 9.9 million deaths in 2020. Conventional treatments for cancer commonly involve mono-chemotherapy or a combination of radiotherapy and mono-chemotherapy. However, the negative side effects of these approaches have been extensively reported and have prompted the search of new therapeutic drugs. In this context, scientific community started to look for innova-tive sources of anticancer compounds in natural sources, including traditional plants. Currently, numerous studies have evaluated the anticancer properties of natural compounds derived from plants, both in vitro and in vivo. In pre-clinical stages, some promising compounds could be men-tioned, such as the sulforaphane or different phenolic compounds. On the other hand, some phy-tochemicals obtained positive results in clinical stages and were further approved for cancer treatment, such as vinca alkaloids or the paclitaxel.
  • 1.0K
  • 01 Mar 2021
Topic Review
Aryl Hydrocarbon Receptor
The aryl hydrocarbon receptor (AhR) was first identified as the intracellular protein that 14 bound and mediated the toxic effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, dioxin) and 15 dioxin-like compounds (DLCs). Subsequent studies show that the AhR plays an important role in 16 maintaining cellular homeostasis and in pathophysiology and there is increasing evidence that the 17 AhR is a important drug target. The AhR binds structurally diverse compounds including 18 pharmaceuticals, phytochemicals, endogenous biochemicals some of which may serve as 19 endogenous ligands. Classification of DLCs and non-DLCs based on their persistence (metabolism), 20 toxicities, binding to wild-type/mutant AhR and structural similarities have been reported. This 21 review provides data suggesting that ligands for the AhR are selective AhR modulators (SAhRMs) 22 which exhibit tissue/cell-specific AhR agonist and antagonist activities and their functional diversity 23 is similar to selective receptor modulators that target steroid hormone and other nuclear receptors.
  • 1.0K
  • 10 Feb 2021
Topic Review
Riboswitches
Riboswitches reside in the 5'- untranslated region of RNA and regulate genes involved in the homeostasis of molecules or Ions they bind to. Since their discovery at the beginning of this century, some of the riboswitches have been regarded as potential antibacterial targets due to their role in the regulation of the homeostasis of the essential metabolites. The pharmacological potential of such riboswitches is being explored u various approaches which include fragment screening, high-throughput screening and rational ligand design guided by X-ray crystallography.
  • 1.0K
  • 24 Feb 2021
Topic Review
Eucalyptus globulus Leaves in Alzheimer’s Disease
Alzheimer’s disease (AD) is the most common neurodegenerative disorder affecting elderly people worldwide. Currently, there are no effective treatments for AD able to prevent disease progression, highlighting the urgency of finding new therapeutic strategies to stop or delay this pathology. Several plants exhibit potential as source of safe and multi-target new therapeutic molecules for AD treatment. Meanwhile, Eucalyptus globulus extracts revealed important pharmacological activities, namely antioxidant and anti-inflammatory properties, which can contribute to the reported neuroprotective effects.
  • 1.0K
  • 17 Aug 2022
Topic Review
Hydroxycinnamic Acids and Skin Damages/Disorders
Alterations of skin homeostasis are widely diffused in our everyday life both due to accidental injuries, such as wounds and burns, and physiological conditions, such as late-stage diabetes, dermatitis, or psoriasis. These events are locally characterized by an intense inflammatory response, a high generation of harmful free radicals, or an impairment in the immune response regulation, which can profoundly change the skin tissue’ repair process, vulnerability, and functionality. Moreover, diabetes diffusion, antibiotic resistance, and abuse of aggressive soaps and disinfectants following the COVID-19 emergency could be causes for the future spreading of skin disorders. In the last years, hydroxycinnamic acids and derivatives have been investigated and applied in several research fields for their anti-oxidant, anti-inflammatory, and anti-bacterial activities.
  • 1.0K
  • 06 Jul 2021
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