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For the study described herein analogues
2022-01-14

For the study described herein, analogues of CID1792197 (2) were selected for exploration. There are a variety of reasons for this decision. First, the synthetic approach, described hereafter, is modular in nature to rapidly enable the independent modification of either end of the molecule. Second,
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br Gastrointestinal peptides and intestinal health Gastroint
2022-01-14

Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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Starting from commercially available dioxaspiro decan ol was
2022-01-14

Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an W123 catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was obtai
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To effectively evaluate prospective mechanisms by which
2022-01-14

To effectively evaluate prospective mechanisms by which chronic HIV infection induces pulmonary fibrotic changes in humans, we confirmed that predisposition to fibrotic change in older individuals could be mimicked in a mouse model. Hydroxyproline is a nonessential amino na+/ca2+ exchanger required
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Acknowledgements br Introduction The neurotransmitter glycin
2022-01-14

Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is
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br Introduction Lichen forming fungi LFFs have evolved in va
2022-01-14

Introduction Lichen-forming fungi (LFFs) have evolved in various classes, including Arthoniomycetes, Coniocybomycetes, Dothideomycetes, Eurotiomycetes, Lecanoromycetes, Leotiomycetes and Lichinomycetes, in Ascomycota (James et al., 2006, Schoch et al., 2009a, Lumbsch and Rikkinen, 2017, Prieto et
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Overall ABC transporters are hypothesised to prevent the pen
2022-01-14

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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77 9 ICH induced striatal lesion produced
2022-01-14

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino 77 9 transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia (Rao e
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Ionotropic glutamate receptors GluRs are ligand
2022-01-14

Ionotropic glutamate receptors (GluRs) are ligand-gated ion channels that mediate information processing at the majority of excitatory synapses in the brain and participate in such physiological processes as learning and memory, development and maintenance of cellular connections, and pain perceptio
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ZD6474 br Experimental section br Acknowledgments MIN cells
2022-01-14

Experimental section Acknowledgments MIN6 ZD6474 were kindly provided by Dr. Junichi Miyazaki, Osaka University. This research was supported in part by the Ministry of Education, Culture, Sports, Science and Technology of Japan (JP16H05099 and JP18H04609 to K.H., and JP16H06574 to T.U.), SENT
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br Glucose metabolism and diet Glucokinase is
2022-01-14

Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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LbGlcK crystallized as a ligandless dimer in
2022-01-14

LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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AKR D is very highly expressed
2022-01-14

AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv
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br Competing interests br Acknowledgements br Introduction
2022-01-14

Competing interests Acknowledgements Introduction - Factors Regulating Glucose Tolerance Strictly speaking, the incretin effect refers to the amplification of insulin secretion, which occurs when Torin1 synthesis is taken in orally as compared to infused intravenously [1]. Normally, the in
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q
2022-01-13

MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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