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Topic Review
Blood–Brain Barrier Transport of Transferrin and Insulin
Biologics can be re-engineered for blood-brain barrier (BBB) transport as IgG fusion proteins, where the IgG domain is a monoclonal antibody (MAb) that targets an endogenous BBB transporter, such as the insulin receptor (IR) or transferrin receptor (TfR). The IR and TfR at the BBB transport the receptor-specific MAb in parallel with the transport of the endogenous ligand, insulin or transferrin. 
  • 942
  • 29 Mar 2022
Topic Review
Methodologies for the physico-chemical characterization of biopharmaceuticals
Biopharmaceuticals are medicinal products obtained by biotechnological processes using molecular biology methods, which include proteins, sugars, nucleic acids, cells, tissues, used for therapeutic or diagnostic purposes in vivo. Genetically modified plants, animals, or microorganisms are also potentially used to produce biopharmaceuticals.
  • 371
  • 29 Mar 2022
Topic Review
Peimine, an Anti-Inflammatory Compound from Chinese Herbal Extracts
Fritillaria bulbs are used in Traditional Chinese Medicine to treat several illnesses. Peimine (Pm), an anti-inflammatory compound from Fritillaria, is known to inhibit some voltage-dependent ion channels and muscarinic receptors, but its interaction with ligand-gated ion channels remains unexplored.
  • 392
  • 29 Mar 2022
Topic Review
Mango Peel Pectin: Recovery, Functionality and Sustainable Uses
Mango peel is the byproduct of agro-processing and has been used for high value-added components such as polysaccharide biopolymers. Pectin derived from the peel is yet to be exploited to its greatest extent, particularly in terms of its separation and physiochemical properties, which limit its applicability to dietary fiber in culinary applications. The functionality of the mango peel pectin (MPP) strongly depends on the molecular size and degree of esterification which highlight the importance of isolation and characterisation of pectin from this novel resource.
  • 941
  • 29 Mar 2022
Topic Review
Antiarrhythmic Drugs on Antiepileptic Drug Action
Severe cardiac arrhythmias developing in the course of seizures increase the risk of SUDEP (sudden unexpected death in epilepsy). Hence, epilepsy patients with pre-existing arrhythmias should receive appropriate pharmacotherapy. Concomitant treatment with antiarrhythmic and antiseizure medications creates, however, the possibility of drug–drug interactions. This is due, among other reasons, to a similar mechanism of action. Both groups of drugs inhibit the conduction of electrical impulses in excitable tissues.
  • 608
  • 28 Mar 2022
Topic Review
Novel Coumarin-Based Inverse Agonists of GPR55
The G-protein coupled receptor 55 (GPR55) was first described in 1999 and is broadly expressed in different areas of the CNS, such as the frontal cortex or the hippocampus. The discovery of the bioactive lipid lysophosphtatidylinositol (LPI) as endogenous GPR55 agonist led to the receptor’s deorphanization . However, besides LPI, several commercially available as well as endogenous ligands show agonistic or antagonistic activity at the GPR55. Endocannabinoids, 2-arachidonoylglycerol, and delta-9-tetrahydrocannabinol (Δ9-THC) for instance, show strong affinities and activation of GPR55, heating up the discussion about GPR55 as potential third cannabinoid-receptor (CB). Commercially available GPR55 agonists, such as O-1602, and GPR55-antagonists like ML-193 are commonly used in GPR55 research, to evaluate GPR55-specific molecular pathways and effects. Besides these widely used GPR55 ligands, coumarin-derivates show antagonistic coupled to inverse agonistic activities on GPR55-dependent neuroinflammatory processes as reported recently.
  • 485
  • 28 Mar 2022
Topic Review
Tissue-Specific Methylation Biosignatures
Tissue-specific gene methylation events are key to the pathogenesis of several diseases and can be utilized for diagnosis and monitoring. By employing a data-driven approach, researchers establish specific methylation disease profiles to be applied in clinical practice and to understand human pathology. 
  • 343
  • 25 Mar 2022
Topic Review
Stability and Activity of L-ASNases
L-asparaginases (EC 3.5.1.1) are a family of enzymes that catalyze the hydrolysis of L-asparagine to L-aspartic acid and ammonia. These proteins with different biochemical, physicochemical and pharmacological properties are found in many organisms, including bacteria, fungi, algae, plants and mammals. To date, asparaginases from E. coli and Dickeya dadantii (formerly known as Erwinia chrysanthemi) are widely used in hematology for the treatment of lymphoblastic leukemias. 
  • 842
  • 24 Mar 2022
Topic Review
Applications of Cubosomes on Cancers
Cancer is a group of disorders characterized by aberrant gene function and alterations in gene expression patterns. In 2020, it was anticipated that 19 million new cancer cases would be diagnosed globally, with around 10 million cancer deaths. Late diagnosis and interventions are the leading causes of cancer-related mortality. In addition, the absence of comprehensive cancer therapy adds to the burden. Many lyotropic non-lamellar liquid-crystalline-nanoparticle-mediated formulations have been developed in the last few decades, with promising results in drug delivery, therapeutics, and diagnostics. Cubosomes are nano-structured liquid-crystalline particles made of specific amphiphilic lipids in particular proportions. Their ability to encapsulate lipophilic, hydrophilic, and amphiphilic molecules within their structure makes them one of a kind. They are biocompatible, versatile drug carriers that can deliver medications through various routes of administration. Many preclinical studies on the use of cubosomes in cancer treatment and theranostic applications have been conducted. However, before cubosomes may be employed in clinical practice, significant technical advances must be accomplished. 
  • 659
  • 24 Mar 2022
Topic Review
Synthesis of the Coumarin Core
Coumarin compounds are attractive organic compounds with many practical applications. Among them there are compounds with biological activity, pharmaceuticals, agrochemicals, dyes, and optoelectronic materials. For this reason, enormous and continuous attempts were made to develop new synthetic pathways and protocols to facilitate the key cyclization reaction of heterocyclic ring and its regioselective functionalization. Of the numerous proposed reactions for the preparation of coumarins, those based on transition metal catalysts have been frequently used recently. Such processes as intramolecular and intermolecular hydroarylation of alkenes or alkynes can be mentioned among the most effective reactions proceeding via the activation of the C–H bond. Knowledge about the mechanistic foundations of catalytic processes seems to be of significant importance in order to improve them and simplify the conditions. Direct functionalization of the coumarin skeleton seems to be one of the more difficult tasks in recent times.
  • 1.0K
  • 23 Mar 2022
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