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br Concluding remarks Several orphan GPCRs have expression
2021-10-18
Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas
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In summary we have designed and optimized a
2021-10-18
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 demonstr
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Our data for glucose and
2021-10-18
Our data for glucose and insulin tolerance tests indicate that niacin-induced hyperglycemia is proportional to the degree of insulin resistance induced, implying that there is deterioration in islet function with niacin treatment (McCulloch et al., 1991). In this regard, we have demonstrated, for th
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procollagen c proteinase Previously we have shown that the n
2021-10-18
Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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Ubiquitination of GlyRs subunit on plasma
2021-10-18
Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor perhexiline synthesis and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also, the functional
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However it is unclear whether the parent and
2021-10-18
However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic bromodomain inhibitor will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40, Na6
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Introduction Glucocorticoids are released in response to str
2021-10-18
Introduction Glucocorticoids are released in response to stress and play an important role in inflammation, cellular growth, development, body fluid homeostasis, carbohydrate, lipid, and protein metabolism. However, circulating glucocorticoid excess has been associated with a classical phenotype of
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Different from stable transfection transient expression was
2021-10-18
Different from stable transfection, transient expression was also found to yield γ-secretase with robust proteolytic activity []. Co-transfection of all four, but not any three, components of human γ-secretase yielded high expression levels. This observation strongly suggests the co-folding nature o
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br Conclusion br Conflict of interest br Acknowledgements br
2021-10-16
Conclusion Conflict of interest Acknowledgements Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial c
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FFAs are essential nutritional molecules that can also modul
2021-10-16
FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty Palosuran derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled receptors (G
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The relationship between the attention deficit hyperactivity
2021-10-16
The relationship between the attention deficit hyperactivity disorder (ADHD) and H3Rs is supported by several reports (Berlin et al., 2011; Passani, Bacciottini, Mannaioni, & Blandina, 2000; Vohora & Bhowmik, 2012). ADHD is a neurobehavioral disorder with high prevalence in children, with hyperactiv
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br Acknowledgement The work was supported
2021-10-16
6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors
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Metal organic frameworks MOFs have emerged over the
2021-10-16
Metal–organic frameworks (MOFs) have emerged over the past two decades with the potentials to act as promising materials in gas storage, chemical separation, catalyst, magnetism, sensing, and drug delivery etc (Du et al., 2013, Zhou and Kitagawa, 2014). Additionally, the secondary interactions, such
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ICLs represent of all generated DNA adducts for cisplatin
2021-10-16
ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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br Materials and methods br Results To examine the
2021-10-16
Materials and methods Results To examine the time and organ specific effect of normal photoperiod and dark environment on the AS601245 of different SlHXKs and on the enzyme activities, these parameters were determined in different leaf positions of tomato plants. Under control conditions, tra
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