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Topic Review
Histone Deacetylases
Histone acetylation status is considered a potential diagnostic biomarker for depression, while inhibitors of histone deacetylases (HDACs) have garnered interest as novel therapeutics.
  • 524
  • 08 Jun 2021
Topic Review
Histamine H1 Receptor Antagonists
Histamine H1 receptor (H1 receptor) antagonists are widely prescribed medications to treat allergic diseases, while recently it has emerged that they show significant promise as anti-SARS-CoV-2 agents.
  • 1.9K
  • 03 Jun 2021
Topic Review
Highly Selective Antagonist of GluK3 Kainate Receptor Subtype
Kainate receptors belong to the family of glutamate receptors ion channels, which are responsible for the majority of rapid excitatory synaptic transmission in the central nervous system. The therapeutic potential of kainate receptors is still poorly understood, which is also due to the lack of potent and subunit-selective pharmacological tools. In search of selective ligands for the GluK3 kainate receptor subtype, a series of quinoxaline-2,3-dione analogues was synthesized and pharmacologically characterized at selected recombinant ionotropic glutamate receptors. Among them, compound 28 was found to be a competitive GluK3 antagonist with submicromolar affinity and unprecedented high binding selectivity, showing a 400-fold preference for GluK3 over other homomeric receptors GluK1, GluK2, GluK5 and GluA2. 
  • 407
  • 22 Feb 2023
Topic Review
High-Grade Gliomas
High-grade glioma (HGG)'s treatment development is hampered by (1) the blood–brain barrier (BBB), (2) an infiltrative growth pattern, (3) rapid development of therapeutic resistance, and, in many cases, (4) dose-limiting toxicity due to systemic exposure. Convection-enhanced delivery (CED) has the potential to significantly limit systemic toxicity and increase therapeutic index by directly delivering homogenous drug concentrations to the site of disease.
  • 457
  • 05 May 2021
Topic Review
Heterogeneity Sources in Metabolic Dysfunction-Associated Fatty Liver Disease
Non-alcoholic fatty liver disease (NAFLD) is a slowly progressing disease, beginning with isolated liver steatosis that evolves in a subset of patients to non-alcoholic steatohepatitis (NASH), liver fibrosis, cirrhosis and hepatocellular carcinoma (HCC). It was recently proposed to redefine NAFLD to metabolic dysfunction-associated fatty liver disease (MAFLD) in which other known causes of liver disease such as alcohol consumption or viral hepatitis do not need to be excluded. Revised nomenclature envisions speeding up and facilitating anti-MAFLD drug development by means of patient stratification whereby each subgroup would benefit from distinct pharmacological interventions. 
  • 496
  • 24 Jan 2022
Topic Review
Heterocyclic PPAR Ligands for Potential Therapeutic Applications
The family of nuclear peroxisome proliferator-activated receptors (PPARα, PPARβ/δ, and PPARγ) is a set of ligand-activated transcription factors that regulate different functions in the body. Whereas activation of PPARα is known to reduce the levels of circulating triglycerides and regulate energy homeostasis, the activation of PPARγ brings about insulin sensitization and increases the metabolism of glucose. On the other hand, PPARβ when activated increases the metabolism of fatty acids. Further, these PPARs have been claimed to be utilized in various metabolic, neurological, and inflammatory diseases, neurodegenerative disorders, fertility or reproduction, pain, and obesity.
  • 587
  • 08 Nov 2022
Topic Review
Herbal Treatments for Breast Cancer
Breast cancer is a complex disease for which pharmacological treatment does not guarantee success or cure. Plants possess phytochemical components with antioxidant and anti-inflammatory properties, mainly coumarins, flavonoids, alkaloids, and terpenoids. Several studies have demonstrated that bioactive compounds from plants can exert anti-tumor activity through various signaling pathways, such as apoptosis, autophagy, modification of the tumor microenvironment, cell arrest, and the suppression of angiogenesis.
  • 203
  • 13 Oct 2023
Topic Review
Hepatic CYP2E1 in Causal Toxicity and Treatment Options
Cytochrome P450 2E1 (CYP2E1), one of the major metabolizing enzymes in humans, is mainly expressed in the liver. Alcohol and several therapeutic drugs, including acetaminophen, are metabolized by CYP2E1 into toxic compounds. At low levels, these compounds are not detrimental, but higher sustained levels of these compounds can lead to life-long problems such as cytotoxicity, organ damage, and cancer. Furthermore, CYP2E1 can facilitate or enhance the effects of alcohol-drug and drug-drug interactions.
  • 452
  • 13 Sep 2022
Topic Review
Hemorphins
Hemorphins are endogenous peptides that are also known as “non-classical” or “atypical” opioid peptides. They are produced under physiologicalor pathological(inflammation) states by hemoglobin proteolysis. They can be released from almost any of the hemoglobin chains (beta-, kappa-, delta-, or epsilon-chain) except the alpha chain.
  • 356
  • 09 Jul 2021
Topic Review
Heavy Metals Levels in Adolescents
In the Milazzo-Valle del Mela area, the presence of industrial plants and the oil refinery make local residents concerned for their health. For this reason, we evaluated the levels of heavy metals in 226 children aged 12–14 years, living in the 7 municipalities of the area. A control age-matched population (n = 29) living 45 km far from the industrial site was also enrolled. Arsenic, cadmium, chromium, mercury, nickel, and vanadium were analysed in 24 h urine samples, while lead concentration was evaluated in blood samples. A questionnaire regarding life style and risk perception was also administered. Adolescents from Milazzo-Valle del Mela had cadmium levels significantly higher compared to either controls (P < 0.0001) or the reference values of the European Germany Environmental Survey (GerES-IV) and the American National Health and Nutrition Examination Survey (NHANES). Furthermore, children had higher perception of living in a high-risk environment. The present data, for the first time, clearly indicate that adolescents living in Milazzo-Valle del Mela have increased body concentration of cadmium, which may be harmful to human health. These results deserve particular attention by the local and regional government to initiate prevention programmes in this susceptible population.
  • 675
  • 01 Nov 2020
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