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Because of its role in the cleavage of
2021-12-20

Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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NMDARs are glutamate gated ionotropic receptors that are inv
2021-12-20

NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo
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Introduction Osteoclasts are large multinuclear cells
2021-12-20

Introduction Osteoclasts are large, multinuclear adenosine receptor that are responsible for the resorption (breakdown) of bone [1]. Together with osteoblasts, the bone forming cell, they maintain the integrity of the skeleton through constant resorption and repair of bone. Osteoclast precursors o
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br Significance Metabolites present in the
2021-12-20

Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS). I
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It is well known that TLR
2021-12-20

It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the
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br Problem of cellular retention not only affects
2021-12-20

Problem of cellular retention not only affects the cellular activity of the nanoparticles and nanocomplexes but can also have ramifications in their in vivo applications. While inorganic nanoparticles are being developed extensively for detection as well as treatment of different human diseases, i
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br Results and discussion Computer modelling studies suggest
2021-12-20

Results and discussion Computer modelling studies suggested that the endocyclic oxygens in furocoumarin derivatives, such as SB 525334 3a (Fig. 1), could also coordinate metal ions in the HIV-1 IN enzyme active site and inhibit the integration of viral DNA. The coumarin moiety is found in variou
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A pyrimidine class of compounds is of
2021-12-20

A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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Histone demethylases are involved in the transcriptional out
2021-12-20

Histone demethylases are involved in the transcriptional output of the AR and hypoxia signaling pathways, and thus contribute to prostate cancer development [12]. For example, the histone demethylase KDM3A serves as a transcriptional coactivator of HIF1α and AR in regulation of their target genes [1
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Newly identified evidence has put immune
2021-12-20

Newly identified evidence has put immune checkpoint inhibitors into the spotlight. However, even though they have been reported to achieve optimistic outcomes [67], there is still a provocative question about their limitations [68]. The solid evidence above has provided us with translational values
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ANT located in the IMM mediates the exchange of
2021-12-20

ANT, located in the IMM, mediates the exchange of ATP/ADP between the mitochondrial matrix and the intermembrane space (IMS) (Brand et al., 2005; Palmieri and Pierri, 2010). Of the 4 known isoforms, ANT1 is the dominant isoform in the heart (Palmieri and Pierri, 2010). Under physiological conditions
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Nevertheless the frequency of CTCs was higher in patients
2021-12-20

Nevertheless, the frequency of CTCs was higher in patients with metastatic breast cancer, which is to be expected because cancer BAY 87-2243 from the original clone that caused the metastasis probably had features favoring their spread throughout the body. When we take HER2+ CTC counts ≥ 3 as a “st
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Of special interest is that riociguat
2021-12-18

Of special interest is that riociguat and NO donors decreased the phosphorylation of many proteins in human platelets. This aspect is presently under further investigation but a few comments can be made already here. Of the extensive spectrum and diversity of human protein kinases and protein phosph
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Our study expands our current knowledge of Ras
2021-12-18

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
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Studies utilising GPR mice however report
2021-12-18

Studies utilising GPR55−/− mice, however, report different effects of GPR55 on body weight and insulin sensitivity. Genetic deletion of GPR55 appears to have no effect on overall body weight 5, 6, 7. However, one of these studies found increased fat deposition and insulin resistance in GPR55−/− mice
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