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A straightforward synthetic pathway was adopted to
2024-05-23

A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic (-)-Lobeline hydrochloride synthesis in two steps following reported procedures., , , The first step involves chloroacety
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br Role of OCT in
2024-05-23

Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for
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br Discussion Here we show opposing effects of iontophoretic
2024-05-23

Discussion Here, we show opposing effects of iontophoretically administered phenylephrine,aselective α1-AR agonist, on firing of putatively DAergic and non-DAergic neurons recorded in vivo in the VTA of urethane anaesthetized rats. Phenylephrine application caused a relatively weak decrease in fi
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Structure activity relationships biochemical metabolic and m
2024-05-23

Structure–activity relationships [23], [24], [25], [26], biochemical [24], [25], [26], [27], [28], [29], [30], [31], metabolic [19], [27], [28], [29], [30], [31], and molecular [32] investigations have demonstrated that the substrate specificity, as well as other characteristics of T. gondii adenosi
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RO-3 br Conclusions The following are the supplementary data
2024-05-23

Conclusions The following are the supplementary data related to this article. Author contributions Conflict of interest Funding sources This work was supported by the Canadian Institutes of Health Research [grant: MOP-79470]. Introduction Sperm cells undergo a number of physical and
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br Results br Discussion The actin cytoskeleton is a highly
2024-05-23

Results Discussion The Fmoc-Phe-OH cytoskeleton is a highly attractive target for many bacterial toxins, owing to its role in activation and locomotion of immune cells, secretion of humoral response factors, and maintenance of protective barriers at the cellular (sub-membrane cytoskeleton) an
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BTL-105 A high throughput small molecule ACK biochemical inh
2024-05-23

A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found BTL-105 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perform
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Whereas more research is needed to identify the precise mech
2024-05-23

Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the Q-VD(OMe)-OPh that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the b
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N-3-oxo-dodecanoyl-L-Homoserine lactone In this study we fir
2024-05-22

In this study, we first determined whether AIF in bovine LT muscle is expressed and the mitochondria released AIF-mediated apoptosis during postmortem aging. For apoptotic issues, the mitochondrial outer membrane is permeabilized, and AIF translocates to the cytosol and to the nucleus, where it indu
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The activity of MMPs is regulated at the
2024-05-22

The activity of MMPs is regulated at the level of gene transcription or by the enzymatic activation of latent enzymes. Inflammatory cytokines such as interleukin (IL)-1β, tumor necrosis factor (TNF)-α and IL-6 are elevated in synovial fluid, synovium and cartilage in patients with OA, and these cyt
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We also explored the possibility that
2024-05-22

We also explored the possibility that this PKC-θ activating protein could operate on the auto-phosphorylation process of the kinase, a specific event accompanying PKC activation [32]. The heated PKC-θ immunoprecipitate from metaphasic cells was then added to PKC-θ isolated both from interphasic or m
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br Materials and methods br Results and discussion br
2024-05-22

Materials and methods Results and discussion Conclusion The preparation of acrylic nanoparticles as aminosugar carriers could not be achieved by direct functionalization of poly(t-butyl acrylate) particles with saccharide groups. A four-step procedure starting from a protected derivative of
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br Concluding Remarks and Future Perspectives The collective
2024-05-22

Concluding Remarks and Future Perspectives The collective evidence from studies detailing the functions of AMPK in the neuromuscular system, combined with those in DMD, SMA, and DM1 surveyed in the present review, strongly suggests that AMPK is a central mediator of neuromuscular determination,
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AMPK is a central regulator of
2024-05-22

AMPK is a central regulator of cell growth, migration, metabolism, autophagy, and cell polarity [20], [21], [22], [23]. It is highly conserved in eukaryotes and functions as the primary sensor of intracellular adenosine nucleotides [24]. When intracellular ATP levels decrease, AMPK is activated to g
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Kuda et al reported that the activity of aminopeptidase
2024-05-22

Kuda et al. (1997) reported that the activity of aminopeptidase A (ApA) but not aminopeptidase B (ApB) nor aminopeptidase N (ApN) was decreased in plasma from patients with Alzheimer's disease (AD). More recently Puertas et al. (2013) reported that the activities of plasma ApA, ApB, ApN and IRAP wer
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