• Prion diseases are transmissible and result

  2022-04-09

  

  Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in ARM1 receptor lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can f

• uPAR promotes cell associated proteolysis by binding to

  2022-04-09

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• A breakthrough in the understanding of the

  2022-04-09

  

  A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty Bromoenol lactone receptor metabolizing enzyme [92], in the execution of

• In the Medicines for Malaria Venture MMV distributed the Ope

  2022-04-09

  

  In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the

• About of human primary melanomas and

  2022-04-09

  

  About 67% of human primary melanomas and 56% of melanoma metastases display cytoplasmic or nuclear β-catenin accumulation (Xue et al., 2016). Of note, active β-catenin stimulates emergence of metastasizing melanoma in mice harboring BrafV600E or NrasQ61K hyperplasia (Damsky et al., 2011, Delmas et a

• br Materials and methods br Results

  2022-04-09

  

  Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa Imiquimod to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-hex content in the total cell

• Accumulating evidence suggests that the NGF family

  2022-04-09

  

  Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, caspase pathway derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knoc

• br Introduction Regulation of transcription is

  2022-04-09

  

  Introduction Regulation of transcription is a critical event of the embryonic development and epigenetic mechanisms such as histone modifications and DNA methylation appear important in mediating temporal changes, and differences among cells/tissues, of temporary stabilized transcriptomes (Mas et

• br Histamine H R Many

  2022-04-09

  

  Histamine H3R Many of the highlight H3R ligands have been described as suitable pharmacological tools for in vitro or in vivo studies and are designated here. The number of ligands and structural categories is huge, and a number of inclusive reviews of the SAR and properties of H3R ligands have b

• Activity of compound in rat brain

  2022-04-08

  

  Activity of compound 10 in rat TNF-alpha, recombinant murine protein receptor tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstr

• Our study expands our current knowledge of Ras like

  2022-04-08

  

  Our study expands our current knowledge of Ras-like small GTPase molecules involved in TLR-mediated responses in macrophages. We found that steady-state levels of Rap2a mRNA and protein undergo alterations after stimuli with TLR agonists. Although statistically significant, the effect of LPS-induced

• Furthermore the role of GSK in

  2022-04-08

  

  Furthermore, the role of GSK-3 in the pathogenesis of inflammation has been widely documented as it accompanies inflammatory conditions such as diabetes mellitus, mood disorders, Alzheimer’s disease, cancer (Jope et al., 2007), and has been associated with atherothrombotic CVD events. However, anoth

• In plants NO production is one of

  2022-04-08

  

  In plants, NO production is one of the early responses to stress (Tossi, Lamattina, & Cassia, 2009). Usually, NO signal transduction requires the involvement of downstream signaling compounds. We further investigated the effects of cGMP on GSK-3 expression. The data showed that LY83583 (a cGMP inhib

• Using embelin and its analogs as surrogate

  2022-04-08

  

  Using embelin and its analogs as surrogate GPR84 agonists we discovered that GPR84 couples to G12 and G13 signaling pathways in addition to Gi, linking receptor function to Rho/Rac signaling and modulation of the cytoskeleton. In primary human macrophages, GPR84 activation leads to Gβγ signaling, Er

• br Results and discussion br Conclusions In

  2022-04-08

  

  Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10

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