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.
  • 873
  • 10 Feb 2021
Topic Review
Antifungal Susceptibility Testing for Fungi
Invasive fungal infections (IFIs) are associated with high mortality rates and timely appropriate antifungal therapy is essential for good outcomes. Emerging antifungal resistance among Candida and Aspergillus spp., the major causes of IFI, is concerning and has led to the increasing incorporation of in vitro antifungal susceptibility testing (AST) to guide clinical decisions.
  • 748
  • 10 Feb 2021
Topic Review
Solution Nuclear Magnetic Resonance
Solution nuclear magnetic resonance (NMR) spectroscopy is a promising tool in drug discovery. Especially, fragment-based drug discovery (FBDD) has benefited a lot from the NMR development. Multiple candidate compounds and FDA-approved drugs derived from FBDD have been developed with the assistance of NMR techniques. NMR has broad applications in different stages of the FBDD process, which includes fragment library construction, hit generation and validation, hit-to-lead optimization and working mechanism elucidation, etc.
  • 709
  • 09 Feb 2021
Topic Review
Fusarium Cyclodepsipeptide Mycotoxins
Most of the fungi from the Fusarium genus are pathogenic to cereals, vegetables, and fruits, and the products of their secondary metabolism mycotoxins may accumulate in foods and feeds. Non-ribosomal cyclodepsipeptides are one of the main mycotoxin groups and include beauvericins (BEAs), enniatins (ENNs), and beauvenniatins (BEAEs).
  • 868
  • 08 Feb 2021
Topic Review
Memantine
Memantine is effective in blocking excessive activity of NMDA-type glutamate receptors and reduces the progression of dementia and may have benefits after TBI.
  • 628
  • 07 Feb 2021
Topic Review
Aflatoxins in Dogs Fed
The Aflatoxins (AF) are difuranocoumarin compounds produced as secondary metabolites of fungi of the genus Aspergillus spp. following a polyketide path.
  • 491
  • 07 Feb 2021
Topic Review
Bifunctional Beta-Lactam Antibiotics
The molecular structure of β-lactam antibiotics can be modified either to introduce another β-lactam ring (the pharmacophore conferring bactericidal activities to these molecules), or to add other pharmacophores that modify their pharmacological properties and spectrum of action.
  • 1.1K
  • 07 Feb 2021
Topic Review
Human Endogenous Retroviruses
Human endogenous retroviruses (HERV) have been implicated in the pathogenesis of several nervous system disorders including multiple sclerosis and amyotrophic lateral sclerosis. 
  • 545
  • 05 Feb 2021
Topic Review
Insulin
Insulin is used for the treatment of diabetes mellitus, which is characterized by hyperglycemia. Subcutaneous injections are the standard mode of delivery for insulin therapy; however, this procedure is very often invasive, which hinders patient compliance, particularly for individuals requiring insulin doses four times a day. Furthermore, cases have been reported of sudden hypoglycemia occurrences following multidose insulin injections. Such an invasive and intensive approach motivates the quest for alternative, more user-friendly insulin administration approaches. For example, transdermal delivery has numerous advantages, such as prolonged drug release, low variability in the drug plasma level, and improved patient compliance.
  • 1.1K
  • 05 Feb 2021
Topic Review
Phospholipids
Phospholipids are unique and versatile molecules. They are of natural occurrence and the main components in cellular membranes. Arranged as a lipid bilayer, phospholipids play a significant role in the structure and functionality of biological membranes. They are amphiphilic and consist of a hydrophilic headgroup and a lipophilic/hydrophobic tail.
  • 2.2K
  • 04 Feb 2021
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