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The excellent potencies selectivities and improved
2024-11-29
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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br Mechanisms for regulation of intracellular
2024-11-29
Mechanisms for regulation of intracellular cholesterol homeostasis Cells maintain intracellular free cholesterol levels and distribution within stringent tolerances by several mechanisms [55]: (1) uptake of native LDL (the major extracellular carrier of cholesterol) by LDL receptors and modified
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We now present a series of
2024-11-29
We now present a series of findings obtained in heterologous expression systems, brain slices, and living animals that suggest that any interaction between mGlu7 and α1-adrenergic receptors exists, is specific, and is physiologically and behaviourally relevant. Materials and methods Norepinephri
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AMPK is an essential player in adiponectin signaling pathway
2024-11-29
AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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In conclusion the results of this investigation suggest that
2024-11-29
In conclusion, the results of this investigation suggest that the involvement of PGE2 in the pathogenesis of pulpal inflammation and repair may be related to its induction of cAMP production. PGE2-induced cAMP production in dental pulp cells is mediated by binding to the EP2 receptor, activation of
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Phosphodiesterase inhibition increases the intracellular lev
2024-11-29
Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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Furthermore we found up regulated protein and mRNA levels
2024-11-29
Furthermore, we found up-regulated protein and mRNA levels of adenosine kinase in mouse retina with TON. The up-regulation of ADK was previously demonstrated in diabetic retinopathy (Pang et al., 2010). Greater levels of ADK in activated macrophages and microglial cells abrogate the immune response.
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Double immunofluorescence staining of Gas and Axl
2024-11-29
Double immunofluorescence staining of Gas6 and Axl with neuronal specific nuclear protein (NeuN), glial fibrillary acidic protein (GFAP), and ionized calcium-binding adaptor molecule 1 (Iba-1), demonstrated that Gas6 and Axl are expressed by neurons, astrocytes and microglia/macrophages (Fig. 2). In
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In this scenario the receptor tyrosine
2024-11-29
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; Pguanidine hy
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br Diabetes and obesity fit or fat sugar or not
2024-11-29
Diabetes and obesity: fit or fat; sugar or not: the autophagic verdict Type 2 diabetes and obesity are among the most emerging health problems worldwide. The factors that are responsible for the establishment of diabetes include decreased Terfenadine production, rise in adiposity, and an increas
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sphingosine-1-phosphate Production of reactive oxygen specie
2024-11-28
Production of reactive oxygen species (ROS) during RSV infection is one the important ways that neutrophils can injure the lungs [2], [24], [25]. Lipoxygenases are considered as an important source of producing ROS inside the sphingosine-1-phosphate [26]. Several studies have indicated that the 12/1
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selective androgen receptor modulators br Results Four HT es
2024-11-28
Results Four HT esters (butyrate, caprylate, laurate and stearate esters) were chosen as representative compounds of increasing lipophilicity (Fig. 1). We will refer to them as C4HT, C8HT, C12HT and C18HT, respectively. They have been synthesized, purified and characterized according to our previ
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Numerous investigators have shown that RACK has several impo
2024-11-28
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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Trichostatin A br Antifungal resistance what is in a
2024-11-28
Antifungal resistance, what is in a name? Antifungal resistance is an emerging and hot topic in the field of medical mycology. Microbiological resistance is identified by determining minimal inhibitory concentrations (MICs) in vitro for a given antifungal and interpreting this value according to
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br Conclusions br Material and methods br Conflicts of inter
2024-11-28
Conclusions Material and methods Conflicts of interest Acknowledgements Introduction Currently more than 30 human proteins are implicated in a range of degenerative disorders owing to their misfolding and misassembly into various aggregate structures and leading to at least 20 serious
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