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br Functional consequences of ADK regulation on neuronal exc
2023-12-22

Functional consequences of ADK regulation on neuronal excitability Adenosine modulates neuronal excitability via activation of the high affinity A1 or A2A, low-affinity A2B, or low abundance A3 adenosine receptors that feed into a multitude of different neuronal and astrocytic pathways (Blum et a
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Direct inhibition of LO activity by BRP is clearly
2023-12-22

Direct inhibition of 5-LO activity by BRP-187 is clearly evident in cell-free assays using PMNL homogenates and isolated human recombinant 5-LO as enzyme source. In such assays, pure FLAP inhibitors like MK886 are inactive [9], [10], [29], [44]. Wash-out experiments and studies using the nonionic de
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br The cytochrome P enzyme hydroxylase
2023-12-22

The cytochrome P450 enzyme 17α-hydroxylase/17,20-lyase (P450) is involved in the production of the C containing androgen precursors from the C containing steroids such as the pregnanes and progestins (). Steroids such as androstenedione (AD) and dehydroepiandrosterone (DHEA) are therefore synthesi
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br Materials and methods br Results To explore
2023-12-22

Materials and methods Results To explore the potential role of autophagy in drug resistance, we firstly performed immunohistochemistry to compare the Altiratinib of p62 in paired primary, metastatic, and recurrent tumor tissues from 26 ovarian cancer patients. The expression of p62 was reveal
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br Aurora A Aurora B
2023-12-22

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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br Introduction The vacuolar ATPases V ATPases are
2023-12-22

Introduction The vacuolar ATPases (V-ATPases) are ATP-driven proton pumps that play important roles in both normal and disease processes [1], [2], [3], [4], [5]. V-ATPases within cells function in such processes as intracellular membrane traffic, protein processing and degradation, coupled transp
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mt t Given the recent discovery of regions of
2023-12-22

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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Indications that HMGA proteins are involved in regulating th
2023-12-21

Indications that HMGA proteins are involved in regulating the structure and function of large chromatin domains come from the early work of Saitoh and Laemmli [143]. Employing immunolocalization techniques, these workers demonstrated that HMGA1 proteins are co-localized with both histone H1 and the
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Introduction The burden of cardiovascular disease CVD is und
2023-12-21

Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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Derivatives of M that possess either an alkyne or an
2023-12-21

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these membrane transporter to maintain 5-HTR antagonist properties as (+)-M100907 was
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Adenosine is a ubiquitous homeostatic substance released fro
2023-12-21

Adenosine is a ubiquitous homeostatic substance released from most cells, including neurons and glias. Endogenous adenosine acts at four principal G-protein-associated receptor subtypes: A1, A2a, A2b and A3 (Ralevic and Burnstock, 1998). The stimulation of adenosine receptors by extracellular adenos
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As an alternative to chronic receptor blockade we have
2023-12-21

As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify Sulfo-NHS-SS-Biotin adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK fa
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br Improvement of endothelial function The vascular endothel
2023-12-21

Improvement of endothelial function The vascular endothelium is a single layer of A 967079 that lines the inner surface of all blood vessels and the heart. In addition to function as a selective barrier to prevent the diffusion of macromolecules from the blood lumen to the intestinal space, the
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The first rationally designed dual mPGES LO inhibitor
2023-12-21

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic AS1404 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesized
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br Methods br Results br Discussion br Acknowledgements br T
2023-12-21

Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V
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