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Another small compound targeting IBAT has been evaluated in
2021-10-23
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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Through the analysis of various synthetic GPR agonists as re
2021-10-22
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic T 705 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK-87
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Thrilled by these promising results our quest for discoverin
2021-10-22
Thrilled by these promising results, our quest for discovering new PPAR-γ/FFAR1 co-agonists was directed towards exploring the other two new scaffolds. So, in this proposed manuscript, we will describe our efforts regarding the synthesis, biological evaluation and molecular docking studies of the be
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MicroRNAs miRNAs are endogenous small RNA molecules
2021-10-22
MicroRNAs (miRNAs) are endogenous small RNA molecules 20–25 nucleotides in length; they regulate multiple genes by binding to target mRNAs, thereby controlling the stability and translation of protein coding mRNAs (Esteller, 2011, Guo et al., 2010). It has been established that Sodium Nitroprusside
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The progression of HIV varies from patient
2021-10-22
The progression of HIV varies from patient to patient, with some who progress slowly and others who progress much faster. However, CD4+ and CD8+ cell counts are intimately linked in those that are able to suppress the HIV infection (Walker et al., 1986; Saez-Aninon et al., 2007). Depletion of these
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br Medium and long chain fatty acid receptors br Clinical
2021-10-22
Medium- and long-chain fatty gap-27 receptors Clinical studies of ω3 fatty acids Clinical studies have established that dietary intake of ω3 fatty acids should be around 4g/day for treating very high triglyceride levels (≥5.7mmol/L) [36]. Low-dose supplementation with EPA + DHA (400mg/day) or
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In recent years several DPP IV inhibitors have
2021-10-22
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic sr9009 mg with a unique xanthine scaffold developed through high-throughp
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In our study we evaluated adenovirus type Ad
2021-10-22
In our study we evaluated adenovirus type 5 (Ad5) as a vehicle for delivering Cre recombinase in conditional transgenic mouse based on the Cre-loxP system, in order to achieve GlyT1 gene modulation in a specific thalamic region in the adult animal. GlyT1 is a sodium- and chloride-coupled glycine tra
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Taking into account abovementioned vitamin D deficiency
2021-10-22
Taking into account abovementioned, vitamin D3 deficiency effects on synaptic neurotransmission can be considered as targeting both Ca2+-independent and Ca2+-dependent processes. Ca2+-independent action of vitamin D3 deficiency is associated with a decrease in the expression of glutamate and GABA tr
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In a previous study M ykkynen et
2021-10-22
In a previous study (Möykkynen et al., 2003), we reported that ethanol lengthens the time needed for the AMPA receptors to recovery from desensitization in isolated hippocampal neurons. Here, we did not observe any effect of ethanol on recovery from desensitization in recombinant homomeric GluR-D re
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br Acknowledgements This work was
2021-10-22
Acknowledgements This work was supported by the National Institutes of Health [grant number GM024417]. Introduction In mammals, glucose is the major energy substrate supporting conceptus development after 77 9 formation [1,2]. While the equine morula uses similar amounts of pyruvate and gluc
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br Conclusion In conclusion SHP was
2021-10-22
Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to
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Genetic disruption or pharmacologic inhibition of the hepati
2021-10-22
Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co
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Similarly both neofunctionalization and subfunctionalization
2021-10-22
Similarly, both neofunctionalization and subfunctionalization likely occurred for the duplicated proglucagon genes. The change in function of GLP-1 would be a neofunctionalization, however in this case it acquired a redundant function – a function that largely overlaps with glucagon effects in the
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While the apparent complexity of gap junction regulation pre
2021-10-22
While the apparent complexity of gap junction regulation presents challenges, new technologies continue to propel the field forward. Advances in microscopy are increasingly able to capture rapid dynamics at the plasma membrane (e.g., biosensors [67] and lattice light sheet microscopy [100]) and to d
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