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br Regulation of GCK by intrinsic conformational dynamics GC
2021-11-11

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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br Declarations of interest br Acknowledgements This work wa
2021-11-11

Declarations of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81673321, 21506099), the State Key Laboratory of Drug Research (SIMM1705KF-13), the Natural Science Foundation of Jiangsu Province (Grant No. BK20151541), and the Jiangsu Syne
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br Results and discussion The synthesis of core
2021-11-11

Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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br G protein coupled receptor GPR also known as a
2021-11-11

G-protein coupled receptor 40 (GPR40), also known as a free fatty cevimeline receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GPR40 agonist i
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Our biological data also showed that in presence
2021-11-11

Our biological data also showed that, in presence of LEDGF/p75, R or S of glycerol T instead of T4, T8 or T12 loop in the T30695-GQ differently affected the integration activity of the enzyme (Table 2), whereas the position but not the chirality of glycerol T affected the inhibitory efficiency of T3
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In recent years the Hippo signaling pathway has emerged
2021-11-11

In recent years, the Hippo signaling pathway has emerged as an important regulator balancing cell proliferation and differentiation [[5], [6], [7]]. The pathway components, first described in the fruit fly Drosophila melanogaster, are highly conserved across different phyla [6]. The signaling pathwa
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phenylephrine hydrochloride Given the role that activation o
2021-11-10

Given the role that activation of GC-C has in stimulating fluid secretion in the intestine, attempts have been made to exploit this pathway to relieve symptoms of chronic constipation. Currently, an orally administered synthetic ST mimic, linaclotide [29], has been successfully shown to alleviate co
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In this study we also investigated
2021-11-10

In this study, we also investigated the role of GST Triflusal in relation to ASD. In univariable analyses, where the role of each GST gene (i.e., GSTM1, GSTT1, GSTP1) was individually assessed, we did not observe any significant associations between the GST genotypes and ASD. In contrast, a previous
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Pharmacologic approaches of inhibiting GSNOR activity have r
2021-11-10

Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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br Materials and methods br Results br Discussion Neurotrans
2021-11-10

Materials and methods Results Discussion Neurotransmitter uptake is one of the most important aspects of synaptic transmission, it fact, the existence of a specific uptake system is one of the requisites that any neuroactive substance has to cover to be considered a neurotransmitter. It has
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br Methods and materials br Results To examine the fear
2021-11-10

Methods and materials Results To examine the fear conditioning effects of the pre-exposure, drug, and sex factors in the total latency time, a 2 × 3 × 2 three-way ANOVA indicated that PRT062070 significant differences occurred in the drug (F2109 = 14.44, p 0.05) and pre-exposure × sex (F1109
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br Methods br Results and discussion Protein analysis of
2021-11-10

Methods Results and discussion Protein analysis of commonly used cell lines (C6, D54-MG, U87, U251 and STTG1) reveals high Dextran sulfate sodium salt of SXC (Cho and Bannai, 1990, Ye et al., 1999, de Groot et al., 2005, Lyons et al., 2007, Savaskan et al., 2008). Since protein expression can
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Interruption of glucagon signaling pathway targeting glucago
2021-11-10

Interruption of glucagon signaling pathway targeting glucagon receptor (GCGR) by gene knockout, antisense oligonucleotides or specific antagonists induces α-cell hyperplasia and alleviates hyperglycemia and other metabolic symptoms in diabetic animals and patients [[7], [8], [9]]. Here we used a ful
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In the second part of
2021-11-10

In the second part of this study, we investigated the influence of GH on the chpg of the ghrelin receptor, GHSR-1a, at the mRNA and peptide levels in cultured whole follicles. Regulation of the expression of GHSR-1a has a key role in the actions of ghrelin in target tissues. Using RT-PCR and Western
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Ghrelin contains an n octanoylation at its Ser residue Kojim
2021-11-10

Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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