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Topic Review
Nuclear factor-κB in Psoriasis
Nuclear factor-κB (NF-κB) plays a central role in psoriasis and canonical Wnt/β-catenin pathway blunts the immune-mediated inflammatory cascade in psoriasis. Adenosine A2A receptor activation blocks NF-κB and boosts the Wnt/β-catenin signaling. PDRN (Polydeoxyribonucleotide) is a biologic agonist of the A2A receptor and its effects were studied in an experimental model of psoriasis. Psoriasis-like lesions were induced by a daily application of imiquimod (IMQ) on the shaved back skin of mice for 7 days. Animals were randomly assigned to the following groups: Sham psoriasis challenged with Vaseline; IMQ animals challenged with imiquimod; and IMQ animals treated with PDRN (8 mg/kg/ip). An additional arm of IMQ animals was treated with PDRN plus istradefylline (KW6002; 25 mg/kg/ip) as an A2A antagonist. PDRN restored a normal skin architecture, whereas istradefylline abrogated PDRN positive effects, thus pointing out the mechanistic role of the A2A receptor. PDRN decreased pro-inflammatory cytokines, prompted Wnt signaling, reduced IL-2 and increased IL-10. PDRN also reverted the LPS repressed Wnt-1/β-catenin in human keratinocytes and these effects were abolished by ZM241385, an A2A receptor antagonist. Finally, PDRN reduced CD3+ cells in superficial psoriatic dermis. PDRN anti-psoriasis potential may be linked to a “dual mode” of action: NF-κB inhibition and Wnt/β-catenin stimulation.
  • 1.0K
  • 03 Nov 2020
Topic Review
Nuclear Factor Kappa B
NF-κB is a family of five eukaryotic transcription factors, p50, p52, p65 (RelA), RelB and c-Rel, which form 15 different homodimers and heterodimers.
  • 678
  • 09 May 2021
Topic Review
Nuclear Factor Erythroid 2-Related Factor 2
Being a controller of cytoprotective actions, inflammation, and mitochondrial function through participating in the regulation of multiple genes in response to stress-inducing endogenous or exogenous stressors, the transcription factor Nuclear Factor Erythroid 2-Related Factor 2 (NRF2) is considered the main cellular defense mechanism to maintain redox balance at cellular and tissue level. While a transient activation of NRF2 protects normal cells under oxidative stress, the hyperactivation of NRF2 in cancer cells may help them to survive and to adapt under oxidative stress. This can be detrimental and related to cancer progression and chemotherapy resistance. Therefore, inhibition of NRF2 activity may be an effective approach for sensitizing cancer cells to anticancer therapy.
  • 352
  • 14 Jun 2023
Topic Review
Nrf2-Keap1-ARE Signaling and IRI
Ischemia/reperfusion (I/R) injury is associated with substantial clinical implications, including a wide range of organs such as the brain, kidneys, lungs, heart, and many others. I/R injury (IRI) occurs due to the tissue injury following the reestablishment of blood supply to ischemic tissues, leading to enhanced aseptic inflammation and stimulation of oxidative stress via reactive oxygen and nitrogen species (ROS/RNS). Since ROS causes membrane lipids’ peroxidation, triggers loss of membrane integrity, denaturation of proteins, DNA damage, and cell death, oxidative stress plays a critical part in I/R pathogenesis. Therefore, ROS regulation could be a promising therapeutic strategy for IRI. In this context, Nrf2 (NF-E2-related factor 2) is a transcription factor that regulates the expression of several factors involved in the cellular defense against oxidative stress and inflammation, including heme oxygenase-1 (HO-1). 
  • 846
  • 01 Jun 2021
Topic Review
NRF2-Activating Compounds Bearing α,β-Unsaturated Moiety
The surge of scientific interest in the discovery of Nuclear Factor Erythroid 2 (NFE2)-Related Factor 2 (NRF2)-activating molecules underscores the importance of NRF2 as a therapeutic target especially for oxidative stress. The chemical reactivity and biological activities of several bioactive compounds have been linked to the presence of α,β-unsaturated structural systems. The α,β-unsaturated carbonyl, sulfonyl and sulfinyl functional groups are reportedly the major α,β-unsaturated moieties involved in the activation of the NRF2 signaling pathway. The carbonyl, sulfonyl and sulfinyl groups are generally electron-withdrawing groups, and the presence of the α,β-unsaturated structure qualifies them as suitable electrophiles for Michael addition reaction with nucleophilic thiols of cysteine residues within the proximal negative regulator of NRF2, Kelch-like ECH-associated protein 1 (KEAP1). The physicochemical property such as good lipophilicity of these moieties is also an advantage because it ensures solubility and membrane permeability required for the activation of the cytosolic NRF2/KEAP1 system.
  • 770
  • 02 Sep 2022
Topic Review
Novel Pyridothienopyrimidine Derivatives
The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b–9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. 
  • 541
  • 10 Feb 2022
Topic Review
Novel Psychoactive Substances
Novel psychoactive substances (NPS) represent a severe health risk for drug users. The molecular mechanisms underlying the action of NPS are more complex than expected, with a wide range of overlap among activated receptors and neurotransmitter systems.
  • 433
  • 21 May 2021
Topic Review
Novel Pharmacological Targets of Post-Traumatic Stress Disorders
Post-traumatic stress disorder (PTSD) is a psychopathological condition with a heterogeneous clinical picture that is complex and challenging to treat. Its multifaceted pathophysiology still remains an unresolved question and certainly contributes to this issue. The pharmacological treatment of PTSD is mainly empirical and centered on the serotonergic system. Since the therapeutic response to prescribed drugs targeting single symptoms is generally inconsistent, there is an urgent need for novel pathogenetic hypotheses, including different mediators and pathways.
  • 151
  • 11 Sep 2023
Topic Review
Novel Fucoidan Pharmaceutical Formulations and Their Potential Application
Fucoidan belongs to a family of sulfated, L-fucose-rich polysaccharides found in the cell wall matrix of various species of marine brown algae (Phaeophyta: Laminariaceae, Fucaceae, Chordariaceae and Alariaceae). Fucoidan can also be obtained from sea cucumbers (Holothuroidea: Stichopodidae, Holothuriidae), sea urchin eggs (Echinoidea: Strongylocentrotidae, Arbaciidae) and sea grasses (Cymodoceaceae).
  • 313
  • 01 Aug 2023
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.
  • 484
  • 28 Mar 2022
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