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Topic Review
Amino Acetophenones for Natural Product Analogs
Commercially available aminoacetophenones are used as "Swiss army knife" for the synthesis of a wide variety of natural products analogs with high therapeutic potential. Being short versatile and uses common reactions, the strategy can be explored in the generation of chemical libraries to be screened in the frame of drug discovery processes.   
  • 964
  • 19 Nov 2021
Topic Review
Caspase-1 Inhibition
The inflammatory protease caspase-1 is associated with the release of cytokines. An excessive number of cytokines (a “cytokine storm”) is a dangerous consequence of COVID-19 infection and has been indicated as being among the causes of death by COVID-19. The anti-inflammatory drug colchicine (which is reported in the literature to be a caspase-1 inhibitor) and the corticosteroid drugs, dexamethasone and methylprednisolone, are among the most effective active compounds for COVID-19 treatment.
  • 962
  • 18 Feb 2022
Topic Review
Polymer-Drug Conjugate in Breast and Lung Cancer
Cancer is a chronic disease that is responsible for the high death rate, globally. The administration of anticancer drugs is one crucial approach that is employed for the treatment of cancer, although its therapeutic status is not presently satisfactory. The anticancer drugs are limited pharmacologically, resulting from the serious side effects, which could be life-threatening. Polymer drug conjugates, nano-based drug delivery systems can be utilized to protect normal body tissues from the adverse side effects of anticancer drugs and also to overcome drug resistance. They transport therapeutic agents to the target cell/tissue. 
  • 956
  • 29 Mar 2022
Topic Review
Epidermal Growth Factor Receptor
Protein kinases are one of the largest enzyme families. By manipulating the location, activity, and functionality of many proteins via multisite phosphorylation, they regulate a broad spectrum of cellular processes. Numerous critical cancer processes, such as tumor growth, metastasis, neovascularization, and chemotherapy resistance, have been shown to be significantly impacted by them. Protein kinases catalyze the transfer of a phosphate group from ATP to the hydroxy group of an amino acid residue. In cellular and molecular process, protein kinases are indispensable. As a result, they play a crucial part in the growth, dissemination, and survival of tumor cells in humans. Hence, this class of enzymes has drawn significant attention as a potential therapeutic target, with multiple kinase suppressors now receiving FDA approval for different cancer indications.
  • 952
  • 25 Mar 2024
Topic Review
Microbubbles Based Drug Delivery Systems
The blood-brain barrier (BBB) is one of the most selective endothelial barriers that protect the brain and maintains homeostasis in neural microenvironments. This barrier restricts the passage of molecules into the brain, except for gaseous or extremely small hydrophobic molecules. Thus, the BBB hinders the delivery of drugs with large molecular weights for the treatment of brain cancers. Various methods have been used to deliver drugs to the brain by circumventing the BBB; however, they have limitations such as drug diversity and low delivery efficiency. To overcome this challenge, microbubbles (MBs)-based drug delivery systems have garnered a lot of interest in recent years. MBs are widely used as contrast agents and are recently being researched as a vehicle for delivering drugs, proteins, and gene complexes. The MBs are 1–10 μm in size and consist of a gas core and an organic shell, which cause physical changes, such as bubble expansion, contraction, vibration, and collapse, in response to ultrasound.
  • 948
  • 20 Apr 2023
Topic Review
Dendrimer–Protein Interactions
Proteins perform vital functions in the cell and in the whole organism. They participate in the transport of substances across the cell membrane, acting as receptors and structural units. The existence of enzymes ensures the passage of biochemical reactions. The drug administration, pharmacokinetic and pharmacodynamic processes are aligned with protein–drug interactions since the plasma contains more than 2400 proteins. Given the potential biomedical applications of dendrimers, the knowledge of their protein-binding properties, the driving force and mechanism of interactions, composition and characteristics of the formed complexes, dependence of structural and morphological changes in proteins on the dendrimer molecular characteristics is of particular importance.
  • 945
  • 26 Apr 2022
Topic Review
Medicinal Potential of Isoflavonoids
In recent years, there is emerging evidence that isoflavonoids could play an important role in the management of type 2 diabetes mellitus (T2DM) due to their reported pronounced biological effects in relation to multiple metabolic factors associated with diabetes. Hence, in this regard, we have comprehensively reviewed the potential biological effects of isoflavonoids, particularly biochanin A, genistein, daidzein, glycitein, and formononetin on metabolic disorders and long-term complications induced by T2DM in order to understand whether they can be future candidates as a safe antidiabetic agent. Based on in-depth in vitro and in vivo studies evaluations, isoflavonoids have been found to activate gene expression through the stimulation of peroxisome proliferator-activated receptors (PPARs) (α, γ), modulate carbohydrate metabolism, regulate hyperglycemia, induce dyslipidemia, lessen insulin resistance, and modify adipocyte differentiation and tissue metabolism. Moreover, these natural compounds have also been found to attenuate oxidative stress through the oxidative signaling process and inflammatory mechanism. Hence, isoflavonoids have been envisioned to be able to prevent and slow down the progression of long-term diabetes complications including cardiovascular disease, nephropathy, neuropathy, and retinopathy. 
  • 943
  • 28 Sep 2021
Topic Review
Solubility, Dissolution and Permeation Enhancement of Natural Compounds
Natural products are the major sources for drug development because of diversity in their structures. They are isolated molecules obtained from plants, minerals or animal resources and used for a variety of therapeutic purposes of human and animal diseases. Though the utilization of natural drugs is from ancient times, the drugs from natural sources still usually face drawbacks of numerous scientific evidences. Despite this, natural products present the major source of biologically active molecules and play a main role in novel drug discovery. Contrary to this, most natural products do not have characteristics of drugs and their pharmacological use is limited. Some of these characteristics lacking in natural products include low aqueous solubility, decreased dissolution rate, poor permeation and low absorption via biological membranes. The possible techniques for the dissolution/solubility and permeability improvements have been addressed which could enhance the dissolution and permeability up to several times.
  • 943
  • 17 Jun 2022
Topic Review
Anticancer Small-Molecule Agents Targeting Eukaryotic Elongation Factor 1A
Eukaryotic elongation factor 1A (eEF1A) canonically delivers amino acyl tRNA to the ribosomal A site during the elongation stage of protein biosynthesis. Yet paradoxically, the oncogenic nature of this instrumental protein has long been recognized. Consistently, eEF1A has proven to be targeted by a wide assortment of small molecules with excellent anticancer activity, among which plitidepsin has been granted approval for the treatment of multiple myeloma. Meanwhile, metarrestin is under clinical development for metastatic cancers.
  • 943
  • 15 Mar 2023
Topic Review
Structural Characteristics, Classification, and Nomenclature of Glycosphingolipids
Glycosphingolipids (GSLs) are a glycolipid subtype which plays vital roles in numerous biological processes, cell–cell interactions, as well as oncogenesis and ontogenesis. They are ubiquitous molecules found mostly in cell membranes.
  • 933
  • 11 Sep 2023
Topic Review
Nucleoside Analogs and Coronaviruses
Coronaviruses (CoVs) are positive-sense RNA enveloped viruses, members of the family Coronaviridae, that cause infections in a broad range of mammals including humans. Several CoV species lead to mild upper respiratory infections typically associated with common colds. However, three human CoV (HCoV) species: Severe Acute Respiratory Syndrome (SARS)-CoV-1, Middle East Respiratory Syndrome (MERS)-CoV, and SARS-CoV-2, are responsible for severe respiratory diseases at the origin of two recent epidemics (SARS and MERS), and of the current COronaVIrus Disease 19 (COVID-19), respectively.
  • 926
  • 24 May 2021
Topic Review
Tumor Polyamine-Suppressing Strategy
Several tumor polyamine-suppressing strategies have been developed, as follows. (1) Ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase 1 (AMD1) are important for polyamine synthesis. The α-difluoromethylornithine (DFMO), which acts as an irreversible suicide inhibitor of ODC, has been used to prevent and treat multiple cancers, such as pancreatic cancer, gastric cancer, lung carcinoma, neuroblastoma, endometrial cancer, and osteosarcoma. (2) Highly regulated catabolic pathways are utilized to control the intracellular polyamine pool. The modulation of the polyamine catabolic enzyme produces decreasing polyamine content and induces the generation of toxic compounds. (3) Some inhibitors targeting the polyamine transport system (PTS) can hinder polyamine import and antagonize polyamine uptake. (4) Synthetic polyamines, including polyamine analogs and polyamine conjugates, possess anticancer activity against tumor cells.
  • 923
  • 01 Sep 2022
Topic Review
Antifungal Azoles by Transition Metal Coordination
Coordination compounds featuring one or more antifungal azole (AA) ligands constitute an interesting family of candidate molecules, given their medicinal polyvalence and the viability of drug complexation as a strategy to improve and repurpose available medications.
  • 919
  • 11 Dec 2023
Topic Review
In-Silico Approaches: Neurodegenerative Diseases
Neurodegenerative diseases (ND), including Alzheimer’s (AD) and Parkinson’s Disease (PD), are becoming increasingly more common and are recognized as a social problem in modern societies. These disorders are characterized by a progressive neurodegeneration and are considered one of the main causes of disability and mortality worldwide. Currently, there is no existing cure for AD nor PD and the clinically used drugs aim only at symptomatic relief, and are not capable of stopping neurodegeneration.
  • 912
  • 19 Apr 2021
Topic Review
Nitrogen Heterocycles and NRF2 Activation
Several nitrogen heterocyclic analogues have been applied to clinical practice, and about 75% of drugs approved by the FDA contain at least a heterocyclic moiety. Thus, nitrogen heterocycles are beneficial scaffolds that occupy a central position in the development of new drugs. The fact that certain nitrogen heterocyclic compounds significantly activate the NRF2/ARE signaling pathway and upregulate the expression of NRF2-dependent genes, especially HO-1 and NQO1, underscores the need to study the roles and pharmacological effects of N-based heterocyclic moieties in NRF2 activation. Furthermore, nitrogen heterocycles exhibit significant antioxidant and anti-inflammatory activities. NRF2-activating molecules have been of tremendous research interest due to their therapeutic roles in neuroinflammation and oxidative stress-mediated diseases. 
  • 909
  • 28 Apr 2023
Topic Review
Hypoglycemic Effect of Resveratrol
El resveratrol (RV) es un compuesto polifenólico con propiedades antioxidantes, antiinflamatorias e hipoglucémicas. Varios estudios in vitro y en modelos animales han demostrado los efectos beneficiosos del RV; sin embargo, los resultados en humanos no son concluyentes.
  • 902
  • 25 Jan 2021
Topic Review
Bioactivity of Steroidal Arylidene Derivatives
Steroids constitute a unique class of chemical compounds, playing an important role in physiopathological processes, and have high pharmacological interest. Due to their straightforward preparation and intrinsic chemical reactivity, steroidal arylidene derivatives are important synthetic intermediates for the preparation of other compounds, particularly bearing heterocyclic systems, in addition to their relevant bioactivity with potential pharmacological interest. 
  • 898
  • 29 Apr 2021
Topic Review
Inhibitor-Enzyme Complexes for New Anti-TB Agents
Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis (TB), is the most devastating human pathogen, as confirmed by the latest TB Report published in October.
  • 896
  • 23 Jan 2022
Topic Review
Phaseolus multiflorus var. albus
Phaseolus multiflorus var. albus (Leguminosae), commonly known as “white kidney bean”, is a twining perennial vine whose fruit has been used as a popular food worldwide owing to its high nutritional content, in terms of proteins, carbohydrates, fats, and vitamins.
  • 894
  • 22 Oct 2021
Topic Review
New Marine Xanthones Isolated since 2010
Xanthones are considered polyketide derivatives due to their biosynthetic precursor. They are aromatic oxygenated heterocyclic compounds with a dibenzo-γ-pyrone scaffold, known as 9H-xanthen-9-one.
  • 891
  • 27 Jun 2022
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