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In humans the superior safety profile of lipid associated fo
2024-01-18
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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Similarly compound was prepared from
2024-01-18
Similarly, A-71623 13 was prepared from aldehyde 8d by following similar procedures (Scheme 3). Condensation of 13 with 7b or 7e provided the corresponding amides 9j or 9k, which then went through O-debenzylation by BCl3 to deliver the final compounds 10j and 10k in 37% and 32% overall yields, resp
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Aldose reductase ALR EC the first enzyme in
2024-01-18
Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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Marimastat In this study we demonstrated that DRR protein le
2024-01-18
In this study, we demonstrated that DRR1 protein level in GBM tissues was significantly higher compared to normal Marimastat tissues. This data suggested that DRR1 might play a role in the tumorigenesis of glioma. To investigate whether DRR1 could accurately predict the outcome in patients with gli
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br ABCA modulates intracellular sphingolipid metabolism
2024-01-18
ABCA2 modulates intracellular sphingolipid metabolism in the LE/LY Recycling of plasma membrane lipids that occurs by constitutive endocytosis and vesicularization of complex glycolipids, complex sphingolipids and cholesterol as well as free cholesterol liberated from LDL after receptor-mediated
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hydroxydopamine OHDA is a selective catecholaminergic neurot
2024-01-18
6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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It has been reported that
2024-01-18
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and
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br Concluding Remarks The effects of
2024-01-18
Concluding Remarks The effects of point mutations of the four ARs on ligand binding affinities, functional potencies, and efficacies constitute a valuable source of pharmacological information. We analyzed the existing data and mapped it on the collection of available AR crystal structures, allo
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Since the localization of LO depends on phosphorylation
2024-01-18
Since the localization of 5-LO depends on phosphorylation, we also analyzed the phosphorylation profile of 5-LO-WT and all isoforms by Western blot using specific Desfuroylceftiofur against the phosphorylation sites S271 and S523. Whereas phosphorylation at S271 activates the 5-LO, inhibits nuclear
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Upregulation of ACLY is common in many cancers Kuhajda
2024-01-17
Upregulation of ACLY is common in many cancers (Kuhajda, 2000, Milgraum et al., 1997, Swinnen et al., 2004, Yahagi et al., 2005). This is in part due to the transcriptional activation by SREBP-1 resulting from the activation of the PI3K/AKT pathway in cancers (Kim et al., 2010, Nadler et al., 2001,
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To the best of our knowledge this
2024-01-17
To the best of our knowledge, this is the first study documenting the SCC modulatory effect at central and kidney level on the shift in the vasoconstrictor-vasodilator ratio of mRNA expression of angiotensin receptors toward vasoconstriction in XY-SCC and/or vasodilation in XX-SCC mice. From these r
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Given that the FST protocol for mice does
2024-01-17
Given that the FST protocol for mice does not engage the exposure to a previous stressful session, posits that Agtr1a levels could be kept higher by basal glutamatergic transmission rather than by stressful stimuli as postulated before. To address this possibility, we used the EMBL-EBI Expression At
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Gallein synthesis Based on structure activity relationship o
2024-01-17
Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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br Perspective AA LA and other PUFAs and their
2024-01-17
Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path
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2 nbdg To verify whether circulating APN could
2024-01-17
To verify whether circulating APN could protect cognitive function during aging, we detected the alterations in circulating adipoenctin levels in aging rats. Our results suggested that circulating APN levels reduced with age. Kawasumi et al’s study results are consistent with ours. They concluded th
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