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A selected set of these new derivatives was
2023-10-13

A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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Previously we described that cadmium induces a more pronounc
2023-10-13

Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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Magnolol In brief serotonin can interact with classes
2023-10-13

In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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The srd a isoforms showed
2023-10-13

The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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br Dihydrotestosterone in adult fish and frogs br New
2023-10-13

Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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AXL is a member of the TAM Tyro Axl Mer
2023-10-13

AXL is a member of the TAM (Tyro3, Axl, Mer) family of receptor tyrosine kinases (RTKs) [4]. Elevated AXL expression could promote oncogenic processes such as cell growth, migration, invasion, and epithelial-to-mesenchymal transition (EMT), which substantially contribute to tumor progression and poo
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However cancer and fibrotic diseases are the most extensivel
2023-10-13

However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX Napabucasin has been reported in breast cancer,, prostate cancer, thyroid cancer, non-s
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It has recently been reported that plasma and
2023-10-13

It has recently been reported that plasma and synovial fluid levels of autotaxin correlate with severity of knee OA. Synovial fibroblasts isolated from OA patients express significant amounts of autotaxin mRNA, and this increase in autotaxin LJI308 receptor could lead to increased production of LPA,
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To test the compounds metabolic stability we measured the
2023-10-13

To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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The surprising finding of our
2023-10-12

The surprising finding of our study is that human M1 macrophages stimulated by LPS express ALOX15B to high levels. So far 12/15-lipoxygenase activity was only reported for IL-4 stimulated anti-phlogistic M2 macrophages [9] but not for the classically activated M1 macrophages. Our data suggest that s
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This project was funded by the University
2023-10-12

This project was funded by the University of the Philippines Diliman through the Natural Sciences Research Institute with grant No. CHE-09-2-02. Introduction There is compelling evidence for an anti-inflammatory effect of 12- and 15-lipoxygenases through the generation of lipid mediators involve
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Given the recent discovery of regions of single
2023-10-12

Given the recent discovery of regions of single-stranded DNA in the nuclei of hypoxic cells, the role for ATR in the response to hypoxic stress seems clearer . Zou and Elledge demonstrated that both Ddc 2 (the homolog of ATRIP) and ATRIP have a lower affinity for double-strand breaks than they do f
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Chromatin proteins play important roles in gene
2023-10-12

Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian Hydroxy Bupropion is transcriptionally silenced by heterochromatin , , , . I
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The first objective of the present
2023-10-12

The first objective of the present study was to investigate the impact of ageing on arginase activity in tissues which exhibit age-related impairments in their function. The second objective was to determine whether l-arginine supplementation modulated the effect of ageing on arginase activity. The
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It is reported that calpain plays a critical role
2023-10-12

It is reported that calpain-2 plays a critical role in BDNF-induced signaling and memory formation, and knockdown of calpain-2, but not calpain-1, completely suppresses BDNF-induced pathway activation and protein translation (Briz et al., 2013). BDNF prevents neuronal apoptosis or death (Ferrer et a
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