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In type diabetic subjects with
2022-02-22

In type-2 diabetic subjects with mean baseline glycated hemoglobin A (HbA) of 8.4%, q.d. administration of MK-0893 for 12weeks as a monotherapy resulted in dose-dependent decreases in HbA and FPG. Administration of MK-0893 q.d. at doses of 20, 40, 60, and 80mg led to observed reductions in HbA of 0.
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Ghrelin is a brain gut peptide
2022-02-22

Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing
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Importantly bioelectric circuits in tissues Fig A have a
2022-02-22

(4) Importantly, bioelectric circuits in tissues (Fig. 2A) have a capacity to store long-term patterning information. An example is planarian anterior-posterior patterning: during regeneration, each fragment cut from a worm needs to build a head and tail at their correct ends. This process is regula
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br Presenilins and apoptosis Apoptosis also known
2022-02-22

Presenilins and apoptosis Apoptosis, also known as programmed cell death, has a critically important role in tissue homeostasis, development, normal ageing and the pathogenesis of several diseases, including cancer and neurological disorders. The presenilins were first linked to apoptosis when ce
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Sulforaphane The schematic diagram of the antagonistic inter
2022-02-22

The schematic diagram of the antagonistic interactions of Zn2+ and neurosteroids (NSs) at GABA-A receptors is summarized in Fig. 7. Neurosteroids exhibit powerful seizure protective effects against experimental seizures probably through the potentiation of synaptic and extrasynaptic GABA-A receptor-
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br Results br Discussion Glucose homeostasis is regulated by
2022-02-21

Results Discussion Glucose homeostasis is regulated by a complex and intricate signaling network involving multiple organs. The BA nuclear receptor FXR is integrated into this regulatory network and participates in glucose handling and metabolism. Intestinal FXR favors glucose Glycyrrhizic aci
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One effective approach to fine tuning the lipophilicity prof
2022-02-21

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Quercitrin scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as Amg
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Due to the presence of all FGFRs in
2022-02-21

Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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br Rationale The present study was motivated to get further
2022-02-21

Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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TRRAP participates in embryonic development as demonstrated
2022-02-21

TRRAP participates in embryonic development, as demonstrated by its binding with proteins regulating the Notch signaling pathway in fruit fly, the Ras signaling pathway in C. elegans, or the Wnt signaling pathway in 293T cells. Therefore we suspect that TRRAP variants, more especially those falling
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devd Distribution of histamine receptors in
2022-02-21

Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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br Conclusions and future perspectives
2022-02-21

Conclusions and future perspectives Declarations of interest Acknowledgements The authors thank Mrs. Kamala Pandey for the help in the preparation of this manuscript. This work was supported by NIH grants R01HL057531 and R01HL062147. Introduction Separation of short exons by long non-co
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The ER is responsible for calcium storage lipid and
2022-02-21

The ER is responsible for calcium storage, lipid and protein biosynthesis, and the folding, assembly, and maturation of proteins [23], and ER stress is one of the main causes in T2DM, which leads to β-cell apoptosis and dysfunction [[5], [6], [7]]. In this study, TG was used as an ER stress inducer.
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With this goal in mind
2022-02-21

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in activ
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Currently ursodeoxycholic acid UDCA is the only recommended
2022-02-21

Currently, ursodeoxycholic HBTU receptor (UDCA) is the only recommended and widely used drug in the treatment of CFLD. However, the clinical efficacy of UDCA is controversial. The most recent Cochrane review only identified a small number of trials assessing the effectiveness of UDCA [92]. The autho
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