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Topic Review
Pyrazole Biomolecules as Cancer and Inflammation Therapeutics
The pyrazole moiety is a heterocyclic ring system (five membered) with 3 C and 2 N in adjacent sites. Pyrazole compounds have an extensive past of applications, being used as herbicides, agrochemicals, and as active pharmaceutical agents. Pyrazole derivatives exhibit anti-inflammatory properties and have been shown to target several cancer cell lines, such as COX (I/II).
  • 2.6K
  • 10 Feb 2023
Topic Review
Strategies for Improving Cell-Penetrating Peptides Stability and Delivery
Peptides play an important role in many fields, including immunology, medical diagnostics, and drug discovery, due to their high specificity and positive safety profile. However, for their delivery as active pharmaceutical ingredients, delivery vectors, or diagnostic imaging molecules, they suffer from two serious shortcomings: their poor metabolic stability and short half-life. Major research efforts are being invested to tackle those drawbacks, where structural modifications and novel delivery tactics have been developed to boost their ability to reach their targets as fully functional species.
  • 2.6K
  • 04 Nov 2022
Topic Review
Theranostic Radiopharmaceuticals
Theranostic Radiopharmaceuticals (Radiotheranostics) is a term in the medical field to define the combination of therapeutic and diagnostic techniques by a suitable radiopharmaceutical agent. Radionuclides are isotopes that emit radiation or have excess nuclear energy, making them chemically unstable and tend to change into another atom. Various types of radiation can be emitted by radionuclides e.g. alpha particles, beta particles, and gamma energy. In radiotheranostics, a pharmaceutical agent (drug) is needed to be a carrier molecule that introduces the radionuclide to its target. Radionuclides are then used as a source of radiation in radiotheranostics that are responsible for diagnosing or treating various diseases.
  • 2.5K
  • 24 May 2022
Topic Review
Pharmacological Properties Improvement by Engineering of Nisin
Nisin is a readily available and cheap lanthipeptide and thus serves as a good model in the search for the tools to engineer lantibiotics with improved pharmacological properties. There are basically two general means to obtain nisin analogs—protein engineering and chemical functionalization of this antibiotic. Although bioengineering techniques have been well developed and enable the creation of nisin mutants of variable structures and properties, they are lacking spectacular effects so far. Chemical modifications of nisin based on utilization of the reactivity of its free amino and carboxylic moieties, as well as reactivity of the double bonds of its dehydroamino acids, are in their infancy.
  • 2.5K
  • 08 Sep 2023
Topic Review
Natural sulfur containing compounds
The present review aims to characterize the general characteristics, physicochemical properties,and health-related studies of onion, garlic, and cruciferous vegetable consumption, as well as theinfluence of food processing on their content of active substances. The review combines distinctchapters where information relevant for nutraceutical and functional food engineers, medical doctors,as well as consumers can be obtained. We believe that the review will stimulate further studies relatedto the implementation of the most accurate sources of sulfur compounds from chosen plants whichcould support the therapy of cancer patients. Moreover, the review aims to present cost-e ectiveanti-tumor means that would include the implementation in the diet of sulfur-based compoundsin foods.
  • 2.5K
  • 26 Aug 2020
Topic Review
Diketopyrrolopyrrole Fluorescent Probes
Diketopyrrolopyrrole (DPP) organic dyes show an exceptional photophysical features (high-fluorescence quantum yield (FQY), good photochemical and thermal stability) that are essential properties for biological applications. This organic dye pigment of DPP is highly effective as it have shown promising results in various applications of AIE, solid-state emission, bio-imaging, cancer therapy and biorecognition of other essential biological components (biomolecules, proteins, enzymes, mitochondria stains) etc. All these results from the DPPs' high fluorescence quantum yield along with its imperatively low-energy fluorescent probe derivatives. Owing to its outstanding photophysical features, in the last decade numerous research papers have been reported with essentially positive results especially for supramolecular chemistry applications. Therefore in a nutshell, this exciting and attractive research area is presently at its infancy, so great efforts needs to be given to it in order to uncover other potentials which might be hidden that are yet to be known to the scientific communities, especially chemists in order to significantly advance it research horizon higher. 
  • 2.4K
  • 27 Mar 2021
Topic Review
Fludeoxyglucose (18F)
Fluorodeoxyglucose (18F) (INN), or fluorodeoxyglucose F 18 (USAN and USP), also commonly called fluorodeoxyglucose and abbreviated [18F]FDG, 18F-FDG or FDG, is a radiopharmaceutical used in the medical imaging modality positron emission tomography (PET). Chemically, it is 2-deoxy-2-[18F]fluoro-D-glucose, a glucose analog, with the positron-emitting radionuclide fluorine-18 substituted for the normal hydroxyl group at the C-2 position in the glucose molecule. The uptake of 18F-FDG by tissues is a marker for the tissue uptake of glucose, which in turn is closely correlated with certain types of tissue metabolism. After 18F-FDG is injected into a patient, a PET scanner can form two-dimensional or three-dimensional images of the distribution of 18F-FDG within the body. Since its development in 1976, 18F-FDG had a profound influence on research in the neurosciences. The subsequent discovery in 1980 that 18F-FDG accumulates in tumors underpins the evolution of PET as a major clinical tool in cancer diagnosis. 18F-FDG is now the standard radiotracer used for PET neuroimaging and cancer patient management. The images can be assessed by a nuclear medicine physician or radiologist to provide diagnoses of various medical conditions.
  • 2.4K
  • 10 Oct 2022
Topic Review
Chemical Enzymology of Monoamine Oxidase
Monoamine oxidase (E.C. 1.4.3.4) enzymes MAO A and MAO B are FAD-containing proteins located on the outer face of the mitochondrial inner membrane, retained there by hydrophobic interactions and a transmembrane helix. The redox co-factor (FAD) is covalently attached to a cysteine and buried deep inside the protein behind an aromatic cage that aligns substrates towards the flavin. MAO metabolizes neurotransmitters such as dopamine and serotonin in the nervous system so is a target for drugs to modify amine levels. MAO also metabolizes a wide range of biogenic amines in all tissues. Current accumulated evidence, particularly from theoretical modelling, supports hydride transfer as the chemical mechanism. The long active site cavity accommodates a wide chemical variety of small molecules designed as inhibitors, including coumarins, chromones, triazoles, and more. Inactivators that bind covalently to MAO include hydrazines, cyclopropylamines and propargylamines. This entry is an extract adapted from a review outlining the remaining uncertainties in the understanding of this key drug target.
  • 2.3K
  • 19 Oct 2021
Topic Review
The Role of Small Molecules Containing Fluorine Atoms
The fluorine atom possesses many intrinsic properties that can be beneficial when incorporated into small molecules. These properties include the atom’s size, electronegativity, and ability to block metabolic oxidation sites. Substituents that feature fluorine and fluorine-containing groups are currently prevalent in drugs that lower cholesterol, relieve asthma, and treat anxiety disorders, as well as improve the chemical properties of various medications and imaging agents. 
  • 2.3K
  • 27 Feb 2024
Topic Review
Roles of the CXCL8-CXCR1/2 Axis in Cancer
In humans, Interleukin-8 (IL-8 or CXCL8) is a granulocytic chemokine with multiple roles within the tumor microenvironment (TME), such as recruiting immunosuppressive cells to the tumor, increasing tumor angiogenesis, and promoting epithelial-to-mesenchymal transition (EMT). 
  • 2.3K
  • 29 Mar 2022
Topic Review
Curcumin: Biochemistry and Antitumoral Action
Curcumin is a pigment with a strong yellow colour found and the main active component of Curcuma longa, a perennial Zingiberaceae plant native to southwest India, but now grown across the South and Southeast Asia, especially in China and India. It is used for centuries as a spice and currently it is viewed as a nutraceutical due to the increasing number of scientific studies demonstrating its anti-oxidant, anti-inflammatory, anti-tumoral and cancer preventive properties. Its chemical structure comprises two aromatic ring systems with o-methoxy phenol groups connected by a seven-carbon linker consisting of an α,β-unsaturated β-diketone with tautomerism when in solution.
  • 2.3K
  • 07 Feb 2021
Topic Review
The Medicinal Chemistry of Artificial Nucleic Acids
Nucleic acids play a central role in human biology, making them suitable and attractive tools for therapeutic applications. While conventional drugs generally target proteins and induce transient therapeutic effects, nucleic acid medicines can achieve long-lasting or curative effects by targeting the genetic bases of diseases.
  • 2.3K
  • 05 Aug 2022
Topic Review
Chemistry of Essential Oils
The term essential oil was created in the 16th century and refers to the theory of “Quinta essentia” proposed by the famous German-Swiss alchemist and physician Paracelsus (1493–1541), born by Theophrastus Philippus Aureolus Bombastus von Hohenheim.
  • 2.3K
  • 13 Oct 2023
Topic Review
Anticancer Effects of Royal Jelly
Royal jelly (RJ) is produced by the hypopharyngeal and mandibular salivary glands of young nurse honeybees. RJ contains bioactive substances, such as carbohydrates, protein, lipids, peptides, mineral salts and polyphenols which contribute to the appreciated biological and pharmacological activities. Antioxidant, anticancer, anti-inflammatory, antidiabetic, and antibacterial impacts are among the well-recognized benefits. The combination of RJ or its constituents with anticancer drugs has synergistic effects on cancer disorders, enhancing the drug’s effectiveness or reducing its side effects. 
  • 2.2K
  • 18 Oct 2022
Topic Review
Mechanism of Self-Healing Hydrogels
Polymeric hydrogels have drawn considerable attention as a biomedical material for their unique mechanical and chemical properties, which are very similar to natural tissues. Among the conventional hydrogel materials, self-healing hydrogels (SHH) are showing their promise in biomedical applications in tissue engineering, wound healing, and drug delivery. Additionally, their responses can be controlled via external stimuli (e.g., pH, temperature, pressure, or radiation). Identifying a suitable combination of viscous and elastic materials, lipophilicity and biocompatibility are crucial challenges in the development of SHH. Furthermore, the trade-off relation between the healing performance and the mechanical toughness also limits their real-time applications. Additionally, short-term and long-term effects of many SHH in the in vivo model are yet to be reported.
  • 2.2K
  • 09 Nov 2022
Topic Review
Small Molecules for Corneal Neovascularization
Multiple natural-source and synthetic small molecules have been tested preclinical for treating corneal neovascularization. Such small molecules include synthetic inhibitors of the vascular endothelial growth factor (VEGF) receptor and other tyrosine kinases, plus repurposed antimicrobials, as well as natural source-derived flavonoid and non-flavonoid phytochemicals, immunosuppressants, vitamins, and histone deacetylase inhibitors.
  • 2.2K
  • 17 Aug 2020
Topic Review
Silver and Silver Nanoparticles for Treatment of COVID-19
COVID-19 is an epizootic and life-threatening outbreak affecting millions of people globally. Coronavirus variants have emerged in different locations since their origin. Silver and its compounds, including silver nanoparticles (AgNPs), have been used in the medical field for a long period, especially in surgical treatments. The anti-microbial and anti-viral properties of silver are well documented. These properties depend on the size of the particles, concentration, precursor, method of preparation, and the presence of other benefiting compounds. Several experiments were conducted by researchers worldwide to prove the anti-bacterial and anti-viral properties of silver (Ag) and AgNPs, emphasizing that silver can be introduced to multiple organs in the human body and exhibit the expected antiviral characteristics.
  • 2.2K
  • 17 Nov 2022
Topic Review
An Overview of PDE4 Inhibitors in Clinical Trials
Since the early 1980s, phosphodiesterase 4 (PDE4) has been an attractive target for the treatment of inflammation-based diseases. Several scientific advancements, by both academia and pharmaceutical companies, have enabled the identification of many synthetic ligands for this target, along with the acquisition of precise information on biological requirements and linked therapeutic opportunities. The transition from pre-clinical to clinical phase was not easy for the majority of these compounds, mainly due to their significant side effects, and it took almost thirty years for a PDE4 inhibitor to become a drug i.e., Roflumilast, used in the clinics for the treatment of chronic obstructive pulmonary disease. Three additional compounds have reached the market: Crisaborole for atopic dermatitis, Apremilast for psoriatic arthritis and Ibudilast for Krabbe disease. 
  • 2.2K
  • 31 Aug 2022
Topic Review
Computational Drug Design of TB
Developing new, more effective antibiotics against resistant Mycobacterium tuberculosis that inhibit its essential proteins is an appealing strategy for combating the global tuberculosis (TB) epidemic. Finding a compound that can target a particular cavity in a protein and interrupt its enzymatic activity is the crucial objective of drug design and discovery. Such a compound is then subjected to different tests, including clinical trials, to study its effectiveness against the pathogen in the host. In recent times, new techniques, which involve computational and analytical methods, enhanced the chances of drug development, as opposed to traditional drug design methods, which are laborious and time-consuming. The computational techniques in drug design have been improved with a new generation of software used to develop and optimize active compounds that can be used in future chemotherapeutic development to combat global tuberculosis resistance.
  • 2.2K
  • 17 Dec 2021
Topic Review
2021 Peptides and Oligonucleotides Harvest
From the medical, pharmaceutical, and social perspectives, 2021 has been a year dominated by the COVID-19 pandemic. However, despite this global health crisis, the pharmaceutical industry has continued its endeavors, and 2021 could be considered an excellent year in terms of the drugs accepted by the US Food and Drug Administration (FDA). Thus, during this year, the FDA has approved 50 novel drugs, of which 36 are new chemical entities and 14 biologics. It has also authorized 10 TIDES (8 peptides, 2 oligonucleotides), in addition to 2 antibody-drug conjugates (ADCs) whose structures contain peptides.
  • 2.2K
  • 17 Feb 2022
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