• A further generally applicable approach for the synthesis

  2022-05-18

  

  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

• Ion dependence of mGluRs activity has been previously

  2022-05-18

  

  Ion dependence of mGluRs activity has been previously reported, notably to Ca2+ and Cl− (Kuang and Hampson, 2006). While mGlu1 and mGlu3 receptors were demonstrated to be sensitive to Ca2+, Cl− modulation was reported for all mGluRs, with a lesser extent for the mGlu2 receptor (DiRaddo et al., 2014;

• In conclusion we provided the first evidence of

  2022-05-18

  

  In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled

• br Material and methods br Results br Discussion Functional

  2022-05-18

  

  Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a

• The in vivo biological activity of

  2022-05-18

  

  The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent

• With the exception of R none

  2022-05-18

  

  With the exception of R5.40310, none of the other residues would appear to be in a position to mediate direct agonist interactions in the active state GLP-1R structures. ECL2 within the GLP-1R is important for affinity and efficacy of both extended and processed GLP-1 peptides [24]. Though distal fr

• The usefulness of GIP R antagonism

  2022-05-18

  

  The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig

• Here we used a designer receptors

  2022-05-18

  

  Here, we used a designer receptors activated exclusively by designer drugs (DREADD)-based chemogenetic approach in a novel Ghsr-IRES-Cre knock-in mouse line to test whether the activity of MBH GHSR neurons is required for the normal rebound food intake following fasting. We also used the Ghsr-IRES-C

• In terms of stimulation oxytocin dopamine noradrenaline adre

  2022-05-18

  

  In terms of stimulation, oxytocin, dopamine, noradrenaline, adrenaline and glucagon have all been reported to increase ghrelin secretion (Mundinger et al., 2006, Iwakura et al., 2011, de la Cour et al., 2007, Gagnon and Anini, 2013). Stimulatory effects on ghrelin secretion have also been observed w

• GSIs were shown to effectively decrease A

  2022-05-18

  

  GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel

• br Methods br Results It is well known that

  2022-05-17

  

  Methods Results It is well known that during the onset of vasoconstriction there is an increase in intracellular Ca2+ which activates myosin light-chain kinase followed by cycling of actin-myosin cross-bridges in VSMCs. Recently, it has been recognized that (-)-Lobeline hydrochloride polymeri

• Although ALPS type is very rare with few

  2022-05-17

  

  Although ALPS type is very rare with few published cases, we herein report the clinical and immunogenetic characteristics of two additional unrelated patients from highly inbred North African population. Both patients present two rare splicing defects mechanisms in FAS gene inducing the skipping of

• Here we show in contrast to previous work that several

  2022-05-17

  

  Here we show, in contrast to previous work, that several phenotypes associated with Orb6 inactivation, including increased cell width, are independent of Gef1. We further find that Orb6 positively regulates exocytosis, also independently of Gef1. To identify novel targets of Orb6, we performed quant

• HIV incidence is often determined

  2022-05-17

  

  HIV incidence is often determined by following cohorts of HIV-uninfected individuals and quantifying the rate of new HIV infections. HIV incidence can also be estimated using a cross-sectional study design, using laboratory assays to identify individuals who are likely to have recent HIV infection.

• It is well known that

  2022-05-17

  

  It is well known that histamine functions not only as an inflammation mediator but also as an aminergic neurotransmitter or neuromodulator. Histaminergic neurons [27], [28] and histamine receptor subtypes (H1R [29] and H3R [30]) are widely existed in mammalian central olfactory system. Histamine reg

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