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The cellular mechanism underlying the
2024-10-12
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Steroidal CYP inhibitors can further be classified based on
2024-10-12
Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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As summarized in Fig autophagy up regulation
2024-10-12
As summarized in Fig. 1, autophagy up-regulation in terms of Beclin 1 induction, increase of LC3 II and p62 down-regulation were observed between 24 and 72 h of cell incubation, this coinciding with the end of the period 27-OH caused slight reduction of cell viability and proliferation as previously
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NOXA a BH only protein is best known as a
2024-10-12
NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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Recently competitive inhibitors of arginase have
2024-10-12
Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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It is noteworthy that in both cases there is a
2024-10-12
It is noteworthy that in both cases there is a higher risk for prematurity [44], [61], [97], [98] and for deliveries of newborn small for GA [89], [95], [97], [98]. sFlt-1:PlGF has been showed to be inversely correlated with GA at birth, since 86% of pregnant women who gave birth at Higher honokiol
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br Acknowledgments and Disclosures br
2024-10-11
Acknowledgments and Disclosures Introduction Over the last decade, the most visible strategy for the treatment of Alzheimer's disease (AD) has been amyloid β peptide (Aβ) immunotherapy (reviewed in [1]). Although the first efforts with Aβ immunotherapy failed to complete clinical trials [1], A
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While there is much in vivo work on prion
2024-10-11
While there is much in vivo work on prion-like Aβ, it has not been shown that one can induce inclusions of Aβ in cultured cells as has been shown for tau and α-synuclein. One reason is practical; Aβ is a low molecular weight metabolite cleaved from within the larger amyloid precursor protein (APP) a
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PF is orally bioavailable and has appropriate pharmacokineti
2024-10-11
PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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With regard to participation of the S lipoxygenase in
2024-10-11
With regard to participation of the 12S-lipoxygenase in diabetes mellitus, inconsistent results have been obtained. Earlier studies demonstrated that the leukocyte-type 12S-lipoxygenase is specifically expressed in pancreatic b-cells and is involved in regulating glucose-stimulated insulin secretion
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Estudos de biomarcadores mostram que
2024-10-11
Estudos de biomarcadores mostram que as concentrações de proteína amiloide no LCR estão inversamente relacionadas com o grau de doença de Alzheimer. No entanto, quer as placas amiloides quer a diminuição da proteína amiloide podem ser encontradas em idosos sem clínica de disfunção cognitiva, pelo qu
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Last decade has provided a
2024-10-11
Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider
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Another open question is whether GABA
2024-10-11
Another open question is whether GABA and ACh are released from the same synaptic vesicles, or even the same presynaptic terminals. Multi-transmitter neurons may either function through co-release, in which multiple neurotransmitters are packaged into the same presynaptic terminal and are therefore
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The anorexic effect observed when AR is infused into
2024-10-11
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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Notably our preliminary results confirmed that
2024-10-11
Notably, our preliminary results confirmed that fluoxetine (SSRIs, 5–10 mg/kg) and duloxetine (SNRIs, 5–10 mg/kg) could not enhance memory function in the novel object recognition or step-down passive avoidance tasks (data not shown). In the present study, we also found that vilazodone showed had no
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