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Topic Review
Mitochondrial Dynamics
Mitochondria are highly dynamic organelles that undergo morphological changes in order to adapt to cellular demands. These changes are orchestrated by the coordinated cycles of fusion and fission, referred to as mitochondrial dynamics, and dysregulation of these processes contributes to disease development. 
  • 1.1K
  • 19 May 2021
Topic Review
Pancreatic Cancer Treatment by Nab-Paclitaxel with Gemcitabine Combination
Pancreatic cancer has one of the highest mortality rates among cancers, and a combination of nab-paclitaxel with gemcitabine remains the cornerstone of first-line therapy. Nab-paclitaxel with gemcitabine in combination with other therapeutic agents can be new treatment strategies in pancreatic cancer. Seven therapeutic agents (ibrutinib, necuparanib, tarextumab, apatorsen, cisplatin, enzalutamide, and momelotinib) are found. 
  • 1.1K
  • 01 Mar 2022
Topic Review
Fluorine-Containing Glycomimetics
Glycomimetics, which are synthetic molecules designed to mimic the structures and functions of natural carbohydrates, have been developed to overcome the limitations associated with natural carbohydrates. The fluorination of carbohydrates has emerged as a promising solution to dramatically enhance the metabolic stability, bioavailability, and protein-binding affinity of natural carbohydrates.
  • 1.1K
  • 26 Sep 2023
Topic Review
Hybrid Azine Derivatives
Infectious diseases caused by microorganisms are a major threat to human health, mostly because of drug resistance, multi-drug resistance and extensive-drug-resistance phenomena to microbial pathogens. During the past, obtaining hybrid azaheterocyclic drugs represents a powerful and attractive approach in modern antimicrobial therapy with very promising results including overcoming microbial drug resistance.
  • 1.1K
  • 01 Dec 2022
Topic Review
Artificial Intelligence for COVID-19 De Novo Drug Design
Artificial intelligence (AI) refers to machines, mainly computers, working like humans. In AI, machines execute tasks such as speech recognition, solving problems, and learning. Machines can work and act like humans if they have enough instruction and knowledge. Drug development is a costly and time-consuming business, and only a minority of approved drugs generate returns exceeding the research and development costs. As a result, there is a huge drive to make drug discovery cheaper and faster. With modern algorithms and hardware, it is not too surprising that the new technologies of artificial intelligence and other computational simulation tools can help drug developers.
  • 1.1K
  • 28 Mar 2022
Topic Review
Pharmacology of LENART01, a Dermorphin–Ranatensin Hybrid Peptide
Diverse chemical and pharmacological strategies are currently being explored to minimize the unwanted side effects of currently used opioid analgesics while achieving effective pain relief. The use of multitarget ligands with activity at more than one receptor represents a promising therapeutic approach.
  • 1.1K
  • 16 Apr 2024
Topic Review
Bisphosphonate-Based Conjugates and Derivatives
Metastatic bone cancer occurs in every type of cancer but is prevalent in lung, breast, and prostate cancers. These metastases can cause extensive morbidity, including a range of skeletal-related events, often painful and linked with substantial hospital resource usage. The treatment used is a combination of chemotherapy and surgery. However, anticancer drugs are still limited because of severe side effects, drug resistance, poor blood supply, and non-specific drug uptake, necessitating high toxic doses. Bisphosphonates are the dominant class of drugs used to inhibit metastatic bone cancer. It is also used to treat osteoporosis and other bone diseases. However, bisphosphonate also suffers from serious side effects. Thus, there is a serious need to develop bisphosphonate conjugates with promising therapeutic outcomes for treating metastatic bone cancer and osteoporosis. This review article focuses on the biological outcomes of designed bisphosphonate-based conjugates for the treatment of metastatic bone cancer and osteoporosis. 
  • 1.0K
  • 09 Jul 2021
Topic Review
Peppers Ethnopharmacology
Piper, Capsicum, and Pimenta are the main genera of peppers consumed worldwide. The traditional use of peppers by either ancient civilizations or modern societies has raised interest in their biological applications, including cytotoxic and antiproliferative effects. 
  • 1.0K
  • 02 Jun 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.
  • 1.0K
  • 29 Sep 2021
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.
  • 1.0K
  • 15 Mar 2023
Topic Review
Triterpenes as Bioactive Natural Products
Natural products (NP) are one of the main sources of diverse pharmacologically active compounds. NPs and NP-scaffolds comprise a large portion of current-day pharmaceutical agents (over 70% of FDA-approved drugs). 
  • 1.0K
  • 11 Jan 2023
Topic Review
HDAC Inhibitors in Triple Negative Breast Cancer
Triple negative breast cancer (TNBC) is an urgent as well as huge medical challenge, which is associated with poor prognosis and responsiveness to chemotherapies. Since epigenetic changes are highly implicated in TNBC tumorigenesis and development, inhibitors of histone deacetylases (HDACIs) could represent a promising therapeutic strategy.
  • 1.0K
  • 01 Jul 2022
Topic Review
Role of Anticancer Drug Glycoconjugates
Sugars, which are a structural element during both the synthesis of the aforementioned glycoconjugates and the preparation of polysaccharide or glycopolymer carriers of anticancer drugs, are widely distributed in nature and also constitute one of the main classes of natural compounds found in living organisms, where they perform important functions in many physiological and pathological processes. 
  • 1.0K
  • 20 Mar 2023
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
New Antimicrobial Oleanonic Acid Polyamine Conjugates
The series of 21 oleanolic acid derivatives containing di- and polyamine fragments at position C3 and C28 was synthesized and evaluated for their antimicrobial activities against both Gram-positive and Gram-negative bacterial. Almost all series presented good to moderate Minimum Inhibitory Concentrations (MIC) against Gram-positive S. aureus, S. faecalis and B. cereus bacteria, moreover compounds possess important antimicrobial activities against Gram-negative E. coli, P. aeruginosa, S. enterica, and EA289 bacteria with MICs ranging from 6.25 to 200 µg/mL. The SAR data showed that the nature of the polyamine fragment, as well as differences in the structure of oleanolic acid plays an important role in the potential activities of tested compounds. The testing of the ability to restore the antibiotic activity of doxycycline and erythromycin at a 2 µg/mL concentration in a synergistic assay showed that only Mannich base with spermine fragment 6 lead to a moderate improvement in terms of antimicrobial activities of the different selected combinations against both P. aeruginosa and E. coli. The study of the mechanism of action of the most important compound in this series (amide 2i derived from N-methyl-norspermidine) showed the effect of disruption of the outer bacterial membrane of P. aeruginosa PA01 cells. Computational ADMET profiling renders compound 2i as a suitable starting point for pharmacokinetic optimization.
  • 1.0K
  • 19 Jan 2022
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.
  • 1.0K
  • 11 Sep 2023
Topic Review
Endogenous Hydrogen Sulfide
Hydrogen sulfide (H2S) is an endogenously produced gaseous signaling molecule and is critical for the regulation of cardiovascular homeostasis.
  • 1.0K
  • 14 Apr 2021
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. 
  • 1.0K
  • 28 Sep 2021
Topic Review
Antimicrobial Effects of Cannabinoids
The development of new antibiotics is urgently needed to combat the threat of bacterial resistance. New classes of compounds that have novel properties are urgently needed for the development of effective antimicrobial agents. The extract of Cannabis sativa L. has been used to treat multiple ailments since ancient times. Its bioactivity is largely attributed to the cannabinoids found in its plant. Researchers are searching for new anti-infective agents that can treat various infections. Although its phytocannabinoid ingredients have a wide range of medical benefits beyond the treatment of infections, they are primarily associated to psychotropic effects. Different cannabinoids have been demonstrated to be helpful against harmful bacteria, including Gram-positive bacteria. Moreover, combination therapy involving the use of different antibiotics has shown synergism and broad-spectrum activity. 
  • 1.0K
  • 31 Oct 2022
Topic Review
Mycomedicine
Mycomedicine is a unique class of natural medicine that has been widely used in Asian countries for thousands of years. Modern mycomedicine consists of fruiting bodies, spores, or other tissues of medicinal fungi, as well as bioactive components extracted from them, including polysaccharides and, triterpenoids, etc.
  • 1.0K
  • 27 Mar 2021
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