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Another lever to efficiently eradicate tumors
2022-02-28
Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing
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In this study according to the critical
2022-02-28
In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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summarizes FAAH inhibition data for a series of benzofuran
2022-02-28
summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibition
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In the present study LLY suppressed the proliferation of
2022-02-28
In the present study, LLY-507 suppressed the proliferation of HGSOC A 967079 via induction of apoptosis. Moreover, the colony-formation assay showed the long-term effects of SMYD2 inhibitors on HGSOC. It has been reported that LLY-507 induces an anti-tumor effect in several types of cancers in vitr
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The H R antagonist cimetidine Tagamet became the first
2022-02-28
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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Expression of p NTR has been
2022-02-28
Expression of p75NTR has been linked to several aspects of aggressive glioma growth, including migration and invasion, by various mechanisms in a large number of elegant studies [6], [7], [26], [27]. Our study adds to this literature by demonstrating specific roles in hypoxic tumor cells and regulat
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br Other Functions of HCA Receptors HCA receptors
2022-02-26
Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor Conoidin A receptor 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in
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Recently we suggested that KYNA
2022-02-26
Recently, we suggested that KYNA – an endogenous GPR35 agonist could be produced in a human cornea since we showed the presence of the enzymes that catalyze the synthesis of KYNA – kynurenine aminotransferases I-III in corneal epithelium, stroma and endothelium (). Therefore, these findings provided
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Recently the novel fatty acid receptor GPR
2022-02-26
Recently, the novel fatty Angiotensin Fragment 1-7 acetate mg receptor, GPR120 (also called FFAR4), has been shown to be implicated in diverse physiological homeostasis, such as insulin sensitization, anti-inflammation and regulation of appetite (Hirasawa et al., 2005, Oh et al., 2010). Notably, it
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Starting from commercially available dioxaspiro decan ol was
2022-02-26
Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an cpt 3 catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was obta
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G protein coupled receptor GPCR ligands can be classified
2022-02-26
G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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Gp induces cell death by apoptotic mechanisms and
2022-02-26
Gp120 induces cell death by apoptotic mechanisms and increases intracellular Ca, and activates messengers related to cell death. Intracellular mechanisms of neuronal damage are mainly a consequence of the activation of the N-methyl-d-aspartate receptor (NMDAR) [2], [5], which induces excitotoxicity
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The HIV genome encodes for a variety of viral
2022-02-26
The HIV-1 genome encodes for a variety of viral proteins necessary for target cell entry and viral replication. gp120 is an HIV-1 envelope glycoprotein that mediates viral particle entry by binding to cell surface receptor CD4 and co-receptors CXCR4 and/or CCR5 depending on viral tropism. While CXCR
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In conclusi http www apexbt
2022-02-26
In conclusion, Glu transactions in glia cells are mediated through Glu receptors and transporters. From a biochemical perspective, the specificity of the cascades has started to be elucidated. A model of our present findings is depicted in Fig. 6. Acknowledgements This work was supported by Gran
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EAAT glutamate uptake is driven by the co
2022-02-26
EAAT glutamate uptake is driven by the co-transport of three sodium ions and one proton, as well as the counter-transport of one potassium ion (Fig. 1B). This complex stoichiometry frees up enough energy to permit phorbol myristate acetate of glutamate into the cell against a steep concentration gr
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