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Molecular properties as well as metabolic
2021-09-28
Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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br Conclusion br Acknowledgments br Introduction The gyloxal
2021-09-28
Conclusion Acknowledgments Introduction The gyloxalase pathway is a well-conserved antioxidant defense system found in all cells of the body [1], [2], [3], [4]. The glyoxalase pathway facilitates the neutralization of highly reactive and oxidizing dicarbonyl molecules, with methylglyoxal (M
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The discovery that GLUT in the microvasculature
2021-09-28
The discovery that GLUT1 in the microvasculature represents an important target of VEGF thereby affecting Fmoc-Asp-OAll function is highly relevant. The work of Jais et al. identified VEGF as a determining player in the regulation of cognitive performance and provides an important link to the unfavo
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We report on four affected children from
2021-09-28
We report on four affected children from two unrelated consanguineous NHS-SS-Biotin with moderate to severe ID associated with epilepsy and variable neuropsychiatric features. Using whole-exome sequencing, we identified homozygous missense variants in SLC45A1 (OMIM: 605763), which codes for a neuron
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Glucagon regulates the transition from hepatic glucose utili
2021-09-28
Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2
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br Glucocorticoid receptor and metabolic syndrome
2021-09-28
Glucocorticoid receptor and metabolic syndrome GCs acting through the GR regulate key enzymes of glucose metabolism in the liver, skeletal muscle, adipose tissue and the pancreas. In the liver, GCs regulate the expression of major gluconeogenic enzymes such as phosphoenolpyruvate carboxykinase, g
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Mitochondria are also involved in other
2021-09-27
Mitochondria are also involved in other modalities of programmed cell death, particularly apoptosis. Intriguingly, the roles of mitochondria in apoptosis and ferroptosis are fundamentally different. In mitochondria-mediated apoptosis, the mitochondrion serves as a reservoir, storing apoptosis-regula
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When taken together data suggest
2021-09-27
When taken together, data suggest CRF plays a central role in linking the HPA axis, the eCB system, and the amygdala with anxiety (Hill et al., 2009, 2010a; Hillard et al., 2011). In elaborate studies in mice, Gray and colleagues (Gray et al., 2015) showed stress-associated increase in CRF concentra
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br HO regulation and physiology The
2021-09-27
HO-1: regulation and physiology The catabolism of cellular heme in humans and other species is mediated by the heme oxygenase (HO) family of enzymes (E.C. 1:14:99:3; heme-hydrogen donor:oxygen oxidoreductase). The HOs localize primarily to the endoplasmic reticulum (ER) where they serve, in conce
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am630 As evidenced by SARs and crystallographic data HO has
2021-09-27
As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer
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br Activation of soluble guanylate cyclase The
2021-09-27
Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple
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br Conclusions br Introduction Astrocytes contribute to phys
2021-09-27
Conclusions Introduction Astrocytes contribute to physiological nigericin sale function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energy
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To date no studies have
2021-09-27
To date, no studies have demonstrated any effect of obesity or inflammation on GPR109A expression in adipose tissue. Our findings demonstrate that HFD-induced obesity decreases adipose tissue GPR109A gene expression. Contradictory to our findings in adipose tissue in vivo, Digby et al. report that e
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Little is known about the
2021-09-27
Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hyperten
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After the synthesis of methylsulfonyl or
2021-09-27
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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