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Glycogen synthase kinase GSK is an evolutionarily conserved
2022-02-21

Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy
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br Pharmacology br Background to GPR
2022-02-21

Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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LPC OMe LPC LPC and OMe LPC were shown to
2022-02-21

LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated V5 Epitope
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Here we demonstrate an anti inflammatory and anticancer
2022-02-21

Here we demonstrate an anti-inflammatory and anticancer function for Gpr109a in colon. Gpr109a signaling imposed anti-inflammatory properties in colonic antigen-presenting cells, which in turn induced differentiation of Treg Aldicarb receptor and IL-10-producing T cells. Gpr109a was also required f
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To overcome these limitations investigators have
2022-02-21

To overcome these limitations, investigators have developed novel strategies for identifying and purifying gonadotropes from transgenic mouse models. For example, FSH-producing gonadotropes have been tagged in vivo with a transgenic cell surface antigen (H-2Kk) so that they can be purified in vitro
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br Conflict of interest statement br Acknowledgements We
2022-02-21

Conflict of interest statement Acknowledgements We acknowledge the support of Zoetis Animal Health, Estrotect, Select Sires and Texas A&M AgriLife Research. The assistance of Randle Franke and Ernest Soto is also gratefully acknowledged. Background Luteal phase deficiency (LPD) is caused b
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br Conclusion br Conflict of interest br
2022-02-18

Conclusion Conflict of interest Acknowledgments This work was supported by an NRF grant (2016R1A2B4011196) from the Korea Research Foundation. Introduction Thymic epithelial tumors are rare, but they are the most common primary neoplasm of the thymus and of the anterosuperior mediastinu
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The SLC A mutations identified in
2022-02-18

The SLC45A1 mutations identified in both families appear to be hypomorphic given that they resulted in a reduction but not abolition of intracellular glucose transport by SLC45A1 in our in vitro assay. It is tempting to speculate that recessive mutations causing a more severe dysfunction of the tran
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The effect of GCK NES mutations on enzyme
2022-02-18

The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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It was previously proposed that glucagon acts in the liver
2022-02-18

It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the VE-822 receptor via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the l
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brompheniramine maleate Following an endoproteolytic cleavag
2022-02-18

Following an endoproteolytic cleavage of C99, γ-secretase trims the remaining fragment Aβ49 or Aβ48 in successive, mostly three-residue steps. Aβ49 typically gives rise to Aβ46, Aβ43, and Aβ40; whereas Aβ48 usually yields Aβ45 and Aβ42 [59]. The physical basis for this characteristic cleavage patter
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RDL is of interest as it
2022-02-18

RDL is of interest as it is the target of highly effective insecticides (Buckingham et al., 2005, Raymond-Delpech et al., 2005). Point mutations, particularly an alanine to serine or glycine mutation in TM2, underlie resistance to several insecticides, including dieldrin, picrotoxinin and fipronil (
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One effective approach to fine tuning the lipophilicity prof
2022-02-18

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic buy ivermectin synthesis scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3
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FGF signals can be transduced to the signaling cascades of
2022-02-18

FGF signals can be transduced to the signaling cascades of RAS-MAPK or PI3K-AKT through FRS2 and GRB2, to the pathways of PKC or PKD via PLCγ and DAG, and to Ca2+-releasing cascade via PLCγ and IP3, finally affecting cellular proliferation, cellular survival, and angiogenesis [48]. By increasing syn
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Recently Bristol Myers Squibb and Merck reported
2022-02-18

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic Nutlin3a derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists wi
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