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Young et al described the
2023-08-15
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Introduction hydroxytryptamine HT is found throughout the bo
2023-08-15
Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary A 61603 hydrobromide (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current
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In the late s Solvay
2023-08-15
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Several dehidropregnenolone derivatives functionalized at C
2023-08-15
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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Introduction Cancer which is responsible for a
2023-08-15
Introduction Cancer, which is responsible for a million deaths each year, is universally feared, and approximately 50% of newly diagnosed cases can be cured [1]. The existing cancer treatments, including surgery, chemotherapy, radiotherapy or a combination of them, are quickly losing efficacy. The
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Imatinib is a well known anticancer drug
2023-08-15
Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing 2365 (K562 cell line
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However joint reviews and the
2023-08-14
However, joint reviews and the consensus from experts offer disparate recommendations with regard to their management in the context of anesthesia, whereas some reviews [6], [7] set out certain doubts regarding their use during the perioperative period. On the other hand, the guidelines for the mana
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It has been proposed that angiotensin II
2023-08-14
It has been proposed that angiotensin II (Ang II) may upregulate COX-2 expression and the subsequent vasoconstrictor prostanoids production through the activation of AT-1 receptors in vascular smooth muscle cells (Hu et al., 2002). Additionally, this peptide is also able to stimulate the generation
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To date attention has been directed towards new molecular ta
2023-08-14
To date, attention has been directed towards new molecular targets in luminal phenotype (ER-positive), such as CDK4/6 and, to a lesser extent, androgen receptor (AR) pathways [8]. While the role of CDK4/6 has been elucidated and their inhibitors have shown a benefit in luminal BC, the role of AR in
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br Concluding remarks Enhanced membrane
2023-08-14
Concluding remarks Enhanced membrane binding upon calcium stimulation in A-1331852 suggests a pre-requisite step that involves a conformational change in LOX. This might facilitate it to tether to the membrane and regulate enzyme activity. The calcium binding loops and the putative active site en
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8-Methoxypsoralen The cavity volume of the binding pocket ma
2023-08-14
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino 8-Methoxypsoralen substitution within a binding pocket may result in a change in the cavity volume. This, in turn,
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br Discussion To our knowledge this is the
2023-08-14
Discussion To our knowledge, this is the first case report that demonstrates the presence of a novel T1151K ALK mutation in a patient with disease progression after crizotinib and then ceritinib. As early as 2011, Zhang et al. identified T1151K among other resistance mutations to crizotinib in Ba
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The study by Lo http
2023-08-14
The study by Lowry et al. (2001) pointed toward functionally uncharacterized DA- and 5-HT-accumulating neurons within the DMH as a potential target for rapid nongenomic effects of CORT. Similar DA- and 5-HT-accumulating systems are distributed throughout the central and peripheral nervous systems, s
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The pathogenesis of d penicillamine induced MG
2023-08-14
The pathogenesis of d-penicillamine-induced MG is not clear. The repertoire of anti-AChR NCT-502 in d-penicillamine-induced MG has been shown to be similar to that in idiopathic MG in terms of AChR antigenic regions, suggesting a common immune mechanism (Tzartos et al., 1988). About 20% of d-penic
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α-mangostin br Thymic expression of AChR Both linear
2023-08-14
Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid follic
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