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br Acknowledgments This research was supported by the
2021-11-26

Acknowledgments This research was supported by the Czech Ministry of Education, Youth and Sports by grants MSM LH11013 and Czech Grant Agency (501/12/0590). David Kopečný and Martina Kopečná were supported by the grant LO1204 from the National Program of Sustainability I by the Ministry of Educat
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In this study we describe the role of a
2021-11-26

In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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br Results and discussion br
2021-11-25

Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p
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Sumatriptan br Experimental br Acknowledgments This project
2021-11-25

Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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Glucose metabolic pathways are well defined but the subcellu
2021-11-25

Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the ras gtpase to respond to physiological changes [1]. Ovadi and Srere have suggested that a new
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The ETB receptor has been shown to
2021-11-25

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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In addition to indoles two additional
2021-11-25

In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic blt2 side chain to prepare compound (). The extension of the chain was expec
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl
2021-11-25

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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Accompanied with apoptosis other ways
2021-11-25

Accompanied with apoptosis, other ways of neuronal death also occur in ischemic SYN-117 due to the impairment of mitochondrial homeostasis [16]. Oxidative DNA damage activates poly (ADP-ribose) polymerase 1 (PARP-1) to induce regulated necrosis, referred to as parthanatos, in the brain [17]. Over-a
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There are several limitations in our
2021-11-25

There are several limitations in our study. First, only the naturally occurring resistance-associated mutations in patients coinfected with HIV/HCV YC 1 australia 1b were analyzed. The result was only applicable to HCV genotype 1b, but not the HCV genotype 1a patients. We did not analyze the effect
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Spindle positioning is governed by the actin cytoskeleton Af
2021-11-25

Spindle positioning is governed by the actin cytoskeleton. After a transient metaphase arrest, cells lacking haspin exhibit a misdistribution of actin, which accumulates within the bud. Actin dynamics is modulated by an intricate network including septins, the polarisome complex, and formins. We sho
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As a measure of ROS formation we measured
2021-11-24

As a measure of ROS formation we measured the extent by which Cu(I) affected the production of hydrogen peroxide and, at the same time, to ensure that there would not be shortage of NADH substrate. Our results show that H2O2 production is increased over time by LPS stimulation but it is not when mic
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Lipid sensing GPCRs as therapeutic targets G protein
2021-11-24

Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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The following are the supplementary data related
2021-11-24

The following are the supplementary data related to this article. Authorship SLC and CGE performed the study conception and experimental design, wrote the paper and directed the activities of this work. ESM and JICA performed most of the degranulation assays, [Ca2+] measurements regarding to the
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In summary the SAR of a series of phenylpropanoic acid
2021-11-24

In summary, the SAR of a series of phenylpropanoic acid-free fatty LB Broth, Miller receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robus
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