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br STAR Methods br AMPK
2024-05-17
STAR★Methods AMPK: A Therapeutic Target in the β Cell? Loss of pancreatic β cell function is a hallmark of the transition to a diagnosis of T2DM (see Glossary) 1, 2, 3, 4. AMPK activation has gained attention for the treatment of hyperglycemia in prediabetes as an insulin-sensitizing agent bec
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Following activation of mGluRs GRIP stabilized AMPARs
2024-05-17
Following activation of mGluRs, GRIP-stabilized AMPARs appear to be the primary target for endocytosis. Consistent with this model, we find that using siRNA to reduce GRIP1/2 expression blocks the AMPAR internalization and the synaptic depression mediated by mGluRs. Reductions in GRIP1/2 expression,
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The lactam emerged as lead candidate due to its
2024-05-17
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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Aldose reductase ALR EC the first enzyme in the
2024-05-17
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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Although several ARIs have reached various phases of
2024-05-17
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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In summary the different types of interstitial cells found i
2024-05-17
In summary, the different types of interstitial cells found in the current study are illustrated in Fig. 7A (see legend for further details), which is suggestive of a heterogeneous complex network of interstitial cells communicating with each other. The possible signaling pathways involving this int
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The results also showed that
2024-05-17
The results also showed that the A3 receptor agonist increased the phosphorylated levels of Akt, leading to activation of the PI3K/Akt pathway. A3 Tideglusib stimulation has protective effects against RGC death following ischemia-reperfusion, glutamate toxicity, and optic nerve transection models (G
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Despite these efforts to prevent oxidative metabolic degrada
2024-05-17
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of
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The myasthenia scale of Millichap and
2024-05-17
The myasthenia scale of Millichap and Dodge was used in our study for ease of comparison of our retrospective data with previous paediatric studies. Our results, with 30% achieving complete remission and 95% achieving at least some degree of clinical improvement following thymectomy, are comparable
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Steroidal CYP inhibitors can further be classified based
2024-05-17
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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The most potent compounds within the
2024-05-17
The most potent compounds within the current series of compounds were therefore , , , , and , with Sodium Orthovanadate possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against th
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Based on currently available knowledge autophagy supports ad
2024-05-16
Based on currently available knowledge, autophagy supports adipocytes development and differentiation. In animals with specific skeletal muscle I-BET 151 hydrochloride synthesis of Atg7, reduced adipogenesis was shown. In rodents, autophagy was decreased in adipose tissue of animals fed with high-f
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Comparison of the GLUT positive plus ACLY
2024-05-16
Comparison of the GLUT1-positive plus ACLY negative group with the GLUT1-negative plus ACLY positive group indicated no significant difference with respect to disease-free survival and overall survival. However, some obvious differences in histological types were found in their formation. A previous
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On the other hand there were only a few cases
2024-05-16
On the other hand, there were only a few cases that expressed DA2R in our study. Additionally, in the cases whose ACTH-secreting pituitary adenomas expressed DA2R, the ratio of positive staining p-Cresyl sulfate was very low. This suggests that dopamine agonists may be less effective in canine Cush
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br Experimental procedures br Results br Discussion Although
2024-05-16
Experimental procedures Results Discussion Although previous studies have indicated that astrocyte aromatase plays a role in nociceptive processes (O'Brien et al., 2015, Smeester et al., 2016), the mechanisms responsible for the regulation of aromatase and its involvement in nociception rem