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Corticosterone induced inhibition of OCT mediated
2023-09-23
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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The anorexic effect observed when AR is
2023-09-22
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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nociceptin receptor We aim to evaluate the AK
2023-09-22
We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of nociceptin receptor injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are high
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A key step in the ADAR reaction is
2023-09-22
A key step in the ADAR reaction is the formation of the adenosine covalent hydrate with a tetrahedral center at C6. The nucleoside analog 8-azanebularine (box in Fig. 6), with its relatively high propensity to form a covalent hydrate, is useful as an adenosine replacement in ADAR2 substrates to trap
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In conclusion we have demonstrated that diaryl pyrazolo
2023-09-22
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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To date the molecular responses
2023-09-22
To date, the molecular responses of AChE have been partially analyzed in its mRNA level or protein activity in aquatic animals. To understand the correlation between transcriptional change and activity of AChE, we conducted both experiments in B. koreanus. Generally, the gnrh agonist patterns of the
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Tacrine an aminoacridine derivative Fig A was the first AChE
2023-09-22
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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The reductase activity in patients with
2023-09-22
The 5α-reductase activity in patients with 21-OHD, as assessed by the 5α-THF to 5β-THF (ratio 3) and by the 5α-17HP to 17HP (ratio 4) ratios, showed a similar pattern of activities (Fig. 2A–C) and significant correlations (ratio 1 vs. ratio 3; rs=0.67; pIn akt pathway to the 5α-reducase activity, th
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GNE-617 Among the most important Ca regulatory mechanisms
2023-09-22
Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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From an historical perspective ligands for GPCRs
2023-09-22
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Azithromycin or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands wer
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br Roles of apelin and APJ
2023-09-22
Roles of apelin and APJ in cardiovascular diseases Therapeutic potential of apelin/APJ in cardiovascular diseases Since the apelin/APJ system plays a key role in the occurrence and development of cardiovascular diseases, it seems logical to presume that targeting this axis should be feasible a
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Anti angiogenic activity of natural products in ocular neova
2023-09-22
Anti-angiogenic activity of natural products in ocular neovascularization A number of molecules, obtained from the natural source, have been evaluated for ocular neovascularization [14], [15]. As these compounds exhibit antioxidant effects, these were also tried for their therapeutic efficacy in in
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Insulin is the central hormone
2023-09-22
Insulin is the central hormone involved in the control of glucose and lipid metabolism. Other nonmetabolic effects of insulin are intensively studied as well. Activation of insulin receptor not only promotes glucose uptake, protein synthesis, and inhibits lipid metabolism, but also is crucial for re
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br Acknowledgments br Introduction Alzheimer s disease AD
2023-09-22
Acknowledgments Introduction Alzheimer's disease (AD) is a severe neurodegenerative disorder primarily affecting the elderly population. Senile plaques in the brain, one of the pathological hallmarks of AD, are formed by the accumulation of aggregated β-amyloid (Aβ) with an extensive β-sheet s
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br AKT signaling is essential during early
2023-09-21
AKT signaling is essential during early dorsal patterning, neural crest induction and maturation AKT signaling modulates EMT and migration of the neural crest cells The defining feature of NC cells is their delamination from the dorsal neural epithelium. At the end of neurulation, mature premi
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