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In recent years there have been further significant
2024-03-30
In recent years, there have been further significant developments that enhance an understanding of the role of adenosine in nociception. Thus, novel methods of recruiting adenosine A1Rs have been developed, and the role of adenosine A2A- and A3Rs in nociception has been further elaborated. Furthermo
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The AChR is composed of five
2024-03-30
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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Having taken a step back
2024-03-29
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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Aurora A or B selective and pan aurora
2024-03-29
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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br ACL A Metabolic Checkpoint for Sensing Excess
2024-03-29
ACL: A Metabolic Checkpoint for Sensing Excess Nutrients? During normal transitions between fasting and feeding, cells maintain energy homeostasis by integrating energy and nutrient status signals at key metabolic nodes, coordinating multiple processes. For example, the AMP-activated protein kina
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Niflumic acid Therefore VEGF and its receptors are expressed
2024-03-29
Therefore, VEGF and its receptors are expressed in different organs, including the kidneys, the liver and the Niflumic acid [55]. In the human placenta, VEGF is mainly synthesized by cytotrophoblast and Hofbauer cells early in the first trimester, whereas Flk-1 and Flt-1 receptors are expressed thr
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We found that decreased Ng levels lead to
2024-03-29
We found that decreased Ng levels lead to a lower threshold for LTD induction at L4–L2/3 synapses. Previous studies in hippocampal slice culture have shown that LTD at individual synapses induces spine elimination at both the targeted synapse and selective neighboring synapses when spines are monito
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The evidence points toward a role for
2024-03-29
The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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Constitutive tyrosine kinase activity of
2024-03-29
Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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In the past years the role of the
2024-03-28
In the past 10 years, the role of the CD73-adenosinergic pathway in suppression of anti-tumor immunity has increasingly been recognized [13], [14]. In this review, we discuss the latest findings dealing with the regulation of anti-tumor immunity by CD73 and adenosine. We also discuss ongoing clinica
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The structure of LO is
2024-03-28
The structure of 5-LO is divided in two domains, the catalytic C-terminal domain and the N-terminal regulatory C2-like domain (C2ld) [59,60]. The C2ld spans the Pentamidine dihydrochloride 1-114 and is responsible for translocation and binding of calcium and membranes [61–63]. The catalytic domain
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Our previous work fails to
2024-03-28
Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef
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Eptifibatide The obtained results indicate that even when
2024-03-28
The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate
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The mechanism by which Gas prevents inflammation
2024-03-28
The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I
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Of the many different types of DNA lesions DNA double
2024-03-28
Of the many different types of DNA lesions, DNA double strand breaks (DSBs) are amongst the most deleterious. It has been suggested that a single unrepaired DSB may be sufficient to induce cell death (Bennett et al., 1993), whereas misrepaired DSBs can result in loss of genetic information, potentia
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