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Multiple studies from our laboratory and others which have
2022-10-04

Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various
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The absence of direct oxidation of Fe by L in
2022-10-04

The absence of direct oxidation of Fe2+ by L1 in experiments in solution would be consistent with the recognized low O2 affinity of sGC. It is known that, in protein phosphatase with other hemoproteins, such as globins and heme-containing oxygenases with a Fe2+-proximal histidine linkage, sGC preve
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Importantly each conformational state in the SRP SR dimer pr
2022-10-04

Importantly, each conformational state in the SRP–SR dimer provides a distinct point of regulation at which these GTPases can directly sense and respond to different biological cues in the pathway. For example, assembly of a stable ‘closed’ complex between SRP and SR is intrinsically very slow (kon
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In summary we have designed
2022-10-04

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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The synthesized methoxyamide derivatives were evaluated for
2022-10-04

The synthesized -methoxyamide derivatives were evaluated for in vitro as GPR119 agonists (, , ) whereas GSK1292263 (II in ) was used as the reference standard. To identify novel sulfone or tetrazole surrogates, diverse functional groups including amide, -sulfonyl amide, hydrazide, -methoxy--methyla
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For a long time the mechanism for the
2022-10-04

For a long time, the mechanism for the TG-lowering effect of nicotinic hippo signaling pathway has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested
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br GnRH receptor expression is altered within GnRH
2022-10-04

GnRH receptor expression is altered within GnRH neuronal cells Kisspeptin failed to stimulate GnRH expression in our line of GT1-7 cells. Instead, we have found that kisspeptin increased the expression of the GnRH receptor in these Talarozole (Sukhbaatar et al., 2013). Based on the results of ex
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Molecular dynamics studies have proved
2022-10-04

Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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br Conclusion Until recently astrocytes were recognized
2022-10-04

Conclusion Until recently, astrocytes were recognized solely for their maintenance role in the regulation of Sephin1 mg homeostasis. Nowadays, this idea has changed, it is clear that these cells play a crucial role in the regulation of neuronal activity and signal transmission. In particular, gl
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Fig A demonstrates the body weight gain
2022-10-04

Fig. 2A demonstrates the body weight gain of the pregestational females. High-fat diet in wild-type mice increased body weight in 2 weeks and sustained this increase over 8 weeks. A similar effect was noted in glut3 mice in response to a high-fat diet. Fig. 2B depicts fat and muscle mass as assessed
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Subsequently we decided to test whether
2022-10-03

Subsequently, we decided to test whether the orexin pathway was involved (Delhanty et al, 2012, Delhanty et al, 2013, Pei et al, 2014). Orexin neuronal systems are known to control limbic and neocortical structures (Bonnavion, de Lecea, 2010, Sakurai, 2007). Orexin receptors and possibly orexin synt
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The release of FBPase and aldolase from
2022-10-02

The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle 1400W dihydrochloride mg was about 6–7 times high
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Previous studies have shown that ox LDL induced hepatic sinu
2022-10-02

Previous studies have shown that ox-LDL-induced hepatic sinus dysfunction is the result of multiple pathways, multi-factorial regulation, and in the present study, we reported for the first time that ox-LDL regulates the basement membrane protein VN through the integrin αvβ5 pathway under high gluco
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The more important effect of pitolisant is related
2022-10-02

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced AZD0156 release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers ref
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Metallothioneins MTs that are intracellular
2022-10-01

Metallothioneins (MTs) that are intracellular proteins responsible for the maintenance of metal homeostasis are involved in arsenic toxicity (Kita et al., 2006). Four major MT isoforms have been reported so far, MT1, MT2A, MT3 and MT4. The synthesis of MT1 and MT2A isoforms in mammal cells can be in
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