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We next considered the effect
2023-09-01

We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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In the search for more specific inhibitors
2023-09-01

In the search for more specific inhibitors of uptake2, Iversen and Salt (1970) speculated that steroids may potentiate the actions of catecholamines on vascular smooth muscle by inhibiting uptake2-mediated catecholamine clearance of the transmitters. They went on to demonstrate that a variety of ste
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br Conflict of interest br
2023-08-31

Conflict of interest Acknowledgments Introduction Inflammation is a protective response of the microcirculation to harmful stimuli. Yet, excessive inflammation is potentially harmful and a characteristic of many chronic diseases [1]. 5-Lipoxygenase (5-LO, EC1.13.11.34) contributes to the in
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To date more than different mutations in
2023-08-31

To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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Thus one possible target for CRPC treatment is
2023-08-31

Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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During preparation of this manuscript some studies investiga
2023-08-31

During preparation of this manuscript, some studies investigating effects of Sunitinib on Axl activity in renal cancer have been published [44], [45], [46], [47]. However, there are several important considerations to take into account interpreting results of these studies. First, Sunitinib doses th
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Aurora A or B selective and
2023-08-31

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 ca
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br Resection of DNA ends
2023-08-31

Resection of DNA ends The highly conserved MRN/MRX complex (Mre11-Rad50-Nbs1 in metazoan; Mre11-Rad50-Xrs2 in yeast) and the Ku70/Ku80 heterodimer (hereafter referred to as Ku) are the first protein complexes to be recruited at DSBs [6]. The presence of Ku and MRN/MRX mediates the recruitment of
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Apelin APJ triggers a variety of
2023-08-31

Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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Atherosclerosis is a chronic lipid
2023-08-31

Atherosclerosis is a chronic lipid metabolism disorder linked with lipid accumulation within the arterial wall and subsequent formation of foam cells and vascular disease [96], [97]. The level of apelin is decreased in human atherosclerotic coronary arteries [4], and coronary collateral formation in
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br Methods and materials br Results br Discussion GPCR regul
2023-08-31

Methods and materials Results Discussion GPCR regulation in response to agonist stimulation is common to nearly all GPCRs and is essential in physiological systems to limit persistent signalling. In this study we have investigated the [Pyr1]apelin-13-induced trafficking and desensitization
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Tunicamycin RNA interference assays have shown that the inhi
2023-08-31

RNA interference assays have shown that the inhibition of AMPK expression leads to increases in TNF-α, IL-6 and cyclooxygenase-2 (COX-2) levels after LPS stimulus, whereas the transfection of macrophages with a constitutively active form of AMPKα1 results in decreased LPS-induced TNF-α and IL-6 prod
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br MHCI peptide editing N terminal extensions and
2023-08-31

MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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Another research group assessed pairs of middle
2023-08-31

Another research group assessed 8503 pairs of middle-aged (CTX0294885 the twin exposed to surgery had lower scores on cognitive tests in 49% of the pairs. Twins aged 70 and older who underwent hip and knee arthroplasty scored higher on cognitive tests, even higher than those who had not undergone an
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Further evidence for action mechanism was provided by assays
2023-08-31

Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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