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Although many GPCR heteromers have been identified using het
2020-11-06
Although many GPCR heteromers have been identified using heterologous cell lines, only very few fit all three criteria. This is mainly due to the difficulties to study these structures in native tissues because of the lack of sensitive and selective tools, not only capable of detecting in vivo evide
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br DGKs inhibition and signaling Local DAG
2020-11-06
DGKs inhibition and signaling Local DAG levels are strictly controlled by a balance between synthesis and degradation rates. Both receptor controlled PLC-mediated production and DGK-mediated degradation are classically implicated in the control of “signaling” DAG. However, this dogma is starting
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Intriguingly our laboratory has shown that
2020-11-06
Intriguingly, our laboratory has shown that the I638F kinase domain mutant, unlike the L63V and G505 mutants, is incapable of receptor autophosphorylation and activation of its downstream effector SHP-2 when exposed to collagen stimulation. These data indicate that I638F is a loss of function mutati
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The DDR mediated lysyl oxidase
2020-11-06
The DDR2-mediated lysyl oxidase induction in osteoblasts reported here is a novel function for this receptor. Various functions have been reported for DDR2. In an in-vitro study, Zhang and colleagues showed that DDR2 activation leads to Runx2 phosphorylation, which regulates osteoblast differentiati
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While lowering the TID exposure of electronics is
2020-11-05
While lowering the TID exposure of electronics is fairly straightforward, there are other Sulindac induced effects that are not as easily mitigated, especially with COTS components. Single Event Effects (SEE) occur when a high-energy particle strikes the active area of an integrated circuit, causing
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br Allosteric inhibitors In general
2020-11-05
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Proinflammatory cytokines induce ER stress in many mammalian
2020-11-05
Proinflammatory cytokines induce ER stress in many mammalian cell systems.32, 33, 34 Our results demonstrate that these cytokines also trigger ER stress in trophoblast JEG-3 cells. However, the severity of stress is likely low grade because only the PERK-EIF2A arm of the UPRER pathway was activated.
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silibinin Third DGK protein stabilization by myristic acid i
2020-11-05
Third, DGKδ2 protein stabilization by myristic silibinin is cell line specific. Myristic acid had no obvious effects on DGKδ protein stability in the liver cell line HepG2, pancreas cell line MIA-PaCa-2 and neuronal cell line Neuro-2a cells (Fig. 5). Although myristic acid moderately increased the
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On the basis of the published
2020-11-05
On the basis of the published articles, it is known that chemokines are produced by leukocytes and tissue cells, constitutively or after induction. Chemokines are responsible for the recruitment of leukocytes to maintain proper functioning of the immune system [14]. They exist in the central nervous
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Wu et al explored the anti
2020-11-05
Wu et al. explored the anti-inflammatory mechanisms by which osthole 35 acted on HepG2 cells cultured in a differentiated medium from cultured 3T3-L1 preadipocyte cells. HepG2 cells, a human liver cell line, were treated with various concentrations of osthole 35 in differentiated media from cultured
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CK comprises a family of
2020-11-05
CK1 comprises a family of serine/threonine protein kinases, that includes different CK1 isoforms namely α, β, δ, ε and γ their various splice variants [56]. It was reported that the pharmacological inhibitor IC261 shows an order of magnitude of higher selectivity for CK1δ or CK1ε isoforms (IC50 of 1
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Introduction Hepatocarcinoma is a common and aggressive form
2020-11-05
Introduction Hepatocarcinoma is a common and aggressive form of cancer (Trad et al., 2017). Due to a high rate of postoperative recurrence and metastasis, the prognosis for HCC remains dismal (Wang et al., 2017a, 2017b). Subclinical metastasis is the major cause responsible for tumor recurrence and
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In the present study we examined whether the gene
2020-11-05
In the present study we examined whether the gene for estrogen receptor alpha, Esr1, plays a role in the expression of maternal memory in female rats. The approach utilized a newly developed rat Esr1 knockout (KO) rat model (Rumi et al., 2014) to evaluate whether deletion of the Esr1 AG-490 affecte
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In normal chow fed mice EP deficiency
2020-11-04
In normal chow fed mice, EP4 deficiency also decreased the expression of CYP8B1, the downstream target of CYP7A1. Similarly, knockdown of EP4 with small interfering RNA reduced the expression of CYP8B1 in HepG2 cells. Therefore, it was anticipated that there would be an increased expression of CYP8B
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br Coactivator Binding Sets APC C
2020-11-04
Coactivator Binding Sets APC/C Catalytic Core in Motion A coactivator not only recruits substrates to APC/C [18] (Figure 3B), but also stimulates repositioning of the catalytic core 19, 24. High-resolution cryo-EM maps of apo forms of APC/C without a coactivator show the catalytic core and platfo
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