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Topic Review
Commercial Targeted Libraries in Drug Design
After the identification of a biological target (enzyme, receptor, protein and so on), the focus of the early phase of drug discovery rests on the identification of leads or compounds that exhibit pharmacological activity against this specific target. Compounds of interest are most often discovered in pre-existing libraries of compounds that can be either virtual or physical. Computer-aided methods which have become increasingly important over the years in drug development utilize virtual compound libraries. While physical compound libraries reach the number of millions of molecules, virtual compound libraries created by large pharmaceutical companies can range from 107 to 1018 molecules. Investigations of these libraries identifies specific molecules, synthetic pathways and focus on a specific chemical space. Targeted libraries are often smaller and are focused towards a specific chemical space. They are created by using relevant biological information with the aim to decrease the processing time associated with larger libraries while maintaining the most relevant chemical space where lead compounds can be found. Due to the fact that they required less computational or wet-lab labor to process they have become very popular with smaller laboratories which try to compete in the drug-development sector. Many modern vendors of compounds today offer such libraries, but the quality of the procedure used to define desired chemical space and select compounds is questionable.
  • 1.2K
  • 25 May 2022
Topic Review
Encapsulate Carotenoids with Cyclodextrin
Carotenoids' inclusion in food matrices presents multiple challenges related to their low stability and low water solubility. The inclusion of carotenoids in complexes with cyclodextrins constitutes a promising technology for the stabilization of these pigments, with possible advantages in terms of their stability in food matrices.
  • 1.2K
  • 10 Jun 2021
Topic Review
Mass Spectrometry Imaging
Mass spectrometry imaging (MSI) or imaging mass spectrometry (IMS) is a promising analytical method to determine and visualize the spatial distribution of specific chemical compositions by their molecular weights or m/z values. MSI is basically a two-dimensional analysis method that can detect intact molecules within tissues or tissue sections without necessitating extraction, purification, and separation.
  • 1.2K
  • 30 Oct 2020
Topic Review
Diabetic Complications: Oxidative Stress/Inflammation
Oxidative stress and inflammation are considered major drivers in the pathogenesis of diabetic complications, including renal and cardiovascular disease. A symbiotic relationship also appears to exist between oxidative stress and inflammation. Several emerging therapies target these crucial pathways, to alleviate the burden of the aforementioned diseases. Oxidative stress refers to an imbalance between reactive oxygen species (ROS) and antioxidant defenses, a pathological state which not only leads to direct cellular damage but also an inflammatory cascade that further perpetuates tissue injury. Emerging therapeutic strategies tackle these pathways in a variety of ways, from increasing antioxidant defenses (antioxidants and Nrf2 activators) to reducing ROS production (NADPH oxidase inhibitors and XO inhibitors) or inhibiting the associated inflamma-tory pathways (NLRP3 inflammasome inhibitors, lipoxins, GLP-1 receptor agonists, and AT-1 re-ceptor antagonists).
  • 1.2K
  • 14 Jan 2021
Topic Review
5-HT2A Receptor Ligands Against Depression
According to the World Health Organization, depression is a multifactorial disorder that affects around 350 million people worldwide. The most widespread monoamine of the CNS-serotonin (5-HT) is believed to play a vital role in the pathomechanism of this condition, and the importance of the neurotransmitter is elevated by the "serotonin hypothesis", linking the presence of the depression-like symptoms with diminished 5-HT concentration in certain brain regions. Serotonin acts its biological effects via numerous receptors. Out of all seven types of serotonin receptors, the serotonin 2A receptor has been identified as a most promising molecular target valuable for the treatment of mood disorders. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel anti-depressants. 
  • 1.2K
  • 14 Feb 2022
Topic Review
Necrotizing Ulcerative Stomatitis
Acute necrotizing ulcerative gingivitis (ANUG) is a common, non-contagious infection of the gums with sudden onset. The main features are painful, bleeding gums, and ulceration of inter-dental papillae (the sections of gum between adjacent teeth). This disease, along with necrotizing (ulcerative) periodontitis (NP or NUP) is classified as a necrotizing periodontal disease, one of the seven general types of gum disease caused by inflammation of the gums (periodontitis). The often severe gum pain that characterizes ANUG distinguishes it from the more common chronic periodontitis which is rarely painful. If ANUG is improperly treated or neglected, it may become chronic and/or recurrent. The causative organisms are mostly anaerobic bacteria, particularly Fusobacteriota and spirochete species. Predisposing factors include poor oral hygiene, smoking, poor nutrition, psychological stress, and a weakened immune system. When the attachments of the teeth to the bone are involved, the term NUP is used. Treatment of ANUG is by removal of dead gum tissue and antibiotics (usually metronidazole) in the acute phase, and improving oral hygiene to prevent recurrence. Although the condition has a rapid onset and is debilitating, it usually resolves quickly and does no serious harm. The informal name trench mouth arose during World War I as many soldiers developed the disease, probably because of the poor conditions and extreme psychological stress.
  • 1.2K
  • 04 Nov 2022
Topic Review
PAMAM Dendrimers
Poly(amidoamine) (PAMAM) dendrimers are repetitively branched, three-dimensional molecules, made of amide and amine subunits, possessing unique physiochemical properties.
  • 1.2K
  • 15 Feb 2022
Topic Review
Cosmopolitodus Hastalis
Cosmopolitodus hastalis, the broad-tooth mako (other common names include the extinct giant mako and broad-tooth white shark), is an extinct mackerel shark that lived from the Miocene epoch to the Pliocene epoch. Its teeth can reach lengths up to 3.5 in (7.5 cm) and are found worldwide. It is believed to be an ancestor to the great white shark, a fact supported by the transitional species Carcharodon hubbelli, and most likely would have been one of the major predators in its ecosystem; preying upon small whales and other mammals.
  • 1.2K
  • 28 Oct 2022
Topic Review
Citrus Breeding 2.0 in Japan
Developing varieties with diverse features that satisfy varied commercial needs, improving overall fruit quality, and quickly releasing them, are prerequisites in citrus breeding. However, these three goals require trade-offs in conventional breeding, even with the application of the marker-assisted selection technique. Conventional breeding cannot achieve these three goals simultaneously and it has been regarded as a breeding trilemma. Integrating a genomics-assisted breeding (GAB) approach that relies on quantitative trait locus detection by genome-wide association study and genome-wide prediction of a trait by genomic selection using enriched marker genotypes enhances breeding efficiency and contributes to eliminating the trilemma. Besides these efforts, the analysis of the genealogy of indigenous citrus varieties revealed that many high-quality indigenous varieties were selected within a few generations. It suggested that selecting a new premium quality hybrid is possible by integrating it with the GAB technique and helps avoid the trilemma. Researchers describe an ongoing comprehensive approach for integrating genomic-assisted breeding (GAB) with citrus genealogy on citrus breeding, called Citrus Breeding 2.0. This method can develop new cultivars with premium quality in a short period.
  • 1.2K
  • 11 Aug 2022
Topic Review
Spix's Macaw
Spix's macaw (Cyanopsitta spixii), also known as the little blue macaw, is a macaw native to Brazil. It is a member of tribe Arini in the subfamily Arinae (Neotropical parrots), part of the family Psittacidae (the true parrots). It was first described by German naturalist Georg Marcgrave, when he was working in the State of Pernambuco, Brazil in 1638 and it is named for German naturalist Johann Baptist von Spix, who collected a specimen in 1819 on the bank of the Rio São Francisco in northeast Bahia in Brazil. The bird is a medium-size parrot weighing about 300 grams (11 oz), smaller than most of the large macaws. Its plumage is various shades of blue, with a grey-blue head, light blue underparts, and vivid blue upperparts. Males and females are almost identical in appearance, however the females are slightly smaller on average. Currently there are no known survivors of the species outside of captivity. The species inhabited riparian Caraibeira (Tabebuia aurea) woodland galleries in the drainage basin of the Rio São Francisco within the Caatinga dry forest climate of interior northeastern Brazil. It had a very restricted natural habitat due to its dependence on the tree for nesting, feeding and roosting. It feeds primarily on seeds and nuts of Caraiba and various Euphorbiaceae (spurge) shrubs, the dominant vegetation of the Caatinga. Due to deforestation in its limited range and specialized habitat, the bird has been rare in the wild throughout the twentieth century. It has always been very rare in captivity, partly due to the remoteness of its natural range. The IUCN regard the Spix's macaw as extinct in the wild. Its last known stronghold in the wild was in northeastern Bahia, Brazil and sightings are very rare. After a 2000 sighting of a male bird, the next and last sighting was in 2016. The species is now maintained through a captive breeding program at several conservation organizations under the aegis of the Brazilian government. It is listed on CITES Appendix I, which makes trade illegal except for legitimate conservation, scientific or educational purposes. The Brazilian Chico Mendes Institute for Biodiversity Conservation (ICMBio) is conducting a project Ararinha-Azul with an associated plan to restore the species to the wild as soon as sufficient breeding birds and restored habitat are available.
  • 1.2K
  • 03 Nov 2022
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