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Acknowledgments br Introduction Prostate cancer is the first
2025-02-21

Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and sign
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br Material and methods br Results br Discussion
2025-02-21

Material and methods Results Discussion Although we were not able to detect 12/15-LOX mRNA in the lungs of 12/15-LOX knockout mice substantial amounts of 15-HETE could be detected in BALF. In fact, significant synthesis of 15-HETE in 12/15-LOX mice have been already reported [17]. The redun
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A high throughput screening campaign led to the discovery
2025-02-21

A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Receptors containing an x y subunit interface where x and
2025-02-21

Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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Molecular docking quantitative structure activity relationsh
2025-02-21

Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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Numerous investigators have shown that RACK has
2025-02-21

Numerous investigators have shown that RACK1 has several important, possibly related, roles in mRNA splicing and in translation. RACK1 interacts directly with specific components of the 40S ribosomal subunit (specifically, the 18S rRNA and ribosomal proteins rpS16e, rpS17e, and rpS3e [new names: uS9
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LOXs and CYPs are a series of iron containing
2025-02-20

LOXs and CYPs are a series of iron-containing enzymes that metabolize arachidonic cyclin-dependent kinase inhibitor to form biologically active products, such as epoxyeicosatrienoic acids (EETs) hydroperoxyeicosatetraenoic acids (HETEs), prostaglandins, leukotrienes and thromboxanes [6]. Among these
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Based on our findings in
2025-02-20

Based on our findings in this work as well as the previous published data in the experimental mice model of RSV infection, we suggest that modulation of 12/15 LOX expression and/or blocking of LOX products such as 12(S)-HETE may represent potential pharmacological approaches to prevent or treat vira
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The specific mechanisms underlying glutamine dependency are
2025-02-20

The specific mechanisms underlying glutamine dependency are still being explored, and current research indicates that the mechanisms likely vary between breast cancer subtypes. In HER2-positive breast cancer, increased levels of the transcriptional activator PGC-1α lead to expression of genes that m
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In our previous study we found that the
2025-02-20

In our previous study we found that the total activity of aldehyde dehydrogenase in cancer SST-14 cyclic peptide of RCC is at the same level as in normal renal tissue [10]. These findings are similar to our results in serum patients with renal cancer. There is no significant difference between ALDH
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The PAS domains of AHR consist of
2025-02-20

The PAS domains of AHR consist of two regions, PAS-A and PAS-B, which function as interfaces for dimerization with ARNT and for ligand binding, respectively [14]. Although both the bHLH and the PAS-A domains have been shown to be involved in dimerization with ARNT, a recent report suggests that only
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Interestingly our transgenic mouse model with macrophages ex
2025-02-20

Interestingly, our transgenic mouse model with macrophages expressing AdipoR1 showed not only improved insulin sensitivity and inflammation in skeletal muscle and adipose tissues, but fat mass, macrophage and plasma lipid accumulation and foam cell formation was also favorably reduced resulting from
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br Endocytosis of AdipoR Surface receptor activity may be sh
2025-02-20

Endocytosis of AdipoR1 Surface receptor activity may be shut down by endocytic uptake and subsequent lysosomal degradation of the proteins [20]. Clathrin-dependent endocytosis (CDE) has been extensively studied and internalization from the plasma membrane is mediated through clathrin-coated pits
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Additionally regulation of GPCR heteromerization by specific
2025-02-20

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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br There is evidence to
2025-02-20

There is evidence to suggest that GMF activities are regulated in vivo by post-translational modification. indeed, there is strong precedent for ADF-homology family proteins being regulated in this manner. Cofilin is inhibited by phosphorylation of a serine residue at its N terminus. This residue
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