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A further generally applicable approach for the synthesis of
2022-03-11

A further generally applicable approach for the synthesis of N-linked glycopeptides involves the convergent Lansbury aspartylation of glycosylamines. Here, the detrimental formation of aspartimides during the activation of the side chain aspartate can be prevented through the use of Ser/Thr pseudopr
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To date glycine receptors have
2022-03-11

To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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Because AM had limited efficacy
2022-03-11

Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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In addition to the increase of extracellular
2022-03-11

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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In conclusion we have designed
2022-03-11

In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date, c
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pterostilbene receptor br Ethics approval br Availability of
2022-03-10

Ethics approval Availability of data and materials Consent for publication Competing interests Authors contributions Introduction Glucose supply to tissues is maintained through a complex regulatory network mostly driven by the pancreatic hormones insulin and glucagon which control
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The effects of C on the
2022-03-10

The effects of C646 on the NF-κB pathway could be explained by the role for p300 that has been described in the regulation of the NF-κB pathway [5]. For instance, acetylations of the p65 NF-κB subunit on lysines 218, 221 and 310 are mediated by the HATs p300 and PCAF [11] and increase transcriptiona
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All of the designed compounds was synth
2022-03-10

All of the designed compounds – was synthesized from -cyclopropane aldehyde , which was prepared following a procedure we reported previously. Treatment of with 4-chlorobenzene-1,2-diamine in pyridine constructed benzimidazole structure of , which was subjected to deprotection and subsequent oxidat
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Betahistine N methyl pyridyl ethylamine is a well known dual
2022-03-10

Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 1186 agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for this indi
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The Hedgehog signaling pathway HH pathway hereafter is vital
2022-03-10

The Hedgehog signaling pathway (HH pathway hereafter) is vital for development and tissue homeostasis. [4] In recent years, studying the role of the HH pathway in carcinogenesis and cancer stemness has highlighted the HH inhibitors as putative cancer therapeutics [5]. However, clinical application o
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In this new therapeutic era nucleic
2022-03-10

In this new therapeutic era, nucleic jtc motors amplification tests (NAATs) remain critically useful. NAATs are recommended to detect HCV RNA in blood following initial serologic diagnosis of HCV infection, to distinguish between spontaneous resolution and progression to chronic infection [7]. In tr
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br Acknowledgments br Introduction Guanosine cyclic monophos
2022-03-10

Acknowledgments Introduction Guanosine 3′,5′-cyclic monophosphate (cGMP) is a signaling molecule with key roles in diverse (patho) physiological responses and processes in numerous prokaryotes and all eukaryotes. The number of reports stating the role of cGMP in different processes in plants i
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br Conclusion Interactions between neurons and
2022-03-10

Conclusion Interactions between neurons and astrocytes depend on the spatial configuration of their contacts. Therefore, changes of astrocyte morphology may impact various physiological mechanisms ranging from glutamate uptake and potassium homeostasis to modulation of synaptic transmission and p
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Toc and Toc are GTPases that regulate
2022-03-10

Toc34 and Toc159 are GTPases that regulate initial steps of preprotein import [3,4,26]. It was shown that GTP hydrolysis of at least one receptor is necessary to initiate the translocation process [23,27]. As reported for other small G-proteins, Toc34 and Toc159 bind their cargo in a nucleotide-depe
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Recent studies on detailed biochemical and structural charac
2022-03-10

Recent studies on detailed biochemical and structural characterization of plant GSNOR AZD 8055 confirmed their similarities to mammalian homologues [16], [17], [18], [19]. Compared to human GSNOR, plant GSNORs exhibit differences in the composition of the anion-binding pocket, which negatively infl
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