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We have previously reported the characterization of A
2020-10-26
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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However with regard to the involvement
2020-10-26
However, with regard to the involvement of PEP in neoplastic processes, few studies and restricted to a very limited number of different tumors have been carried out [4], [18], [19]. Therefore, in order to ascertain the possible role of this enzyme in pathological proliferative tissues, in the prese
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Nitric oxide synthase NOS is a
2020-10-26
Nitric oxide synthase (NOS) is a predominant enzyme of immune system, which elaborates nitric oxide (NO) from the amino Busulfan sale arginine (Arg). NO mediates vasodilatation, blood pressure regulation, neurotransmission, host defense, and macrophage-mediated immunity, among an array of other func
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Third DGK protein stabilization by myristic acid is
2020-10-26
Third, DGKδ2 protein stabilization by myristic Luzindole 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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The homologous DDRs are composed of an N
2020-10-26
The homologous DDRs are composed of an N-terminal discoidin homology domain, followed by a sequence of ∼220 amino acids unique to the DDRs, a transmembrane domain, a large juxtamembrane domain, and a conserved cytoplasmic tyrosine kinase domain. In a previous study, we demonstrated that DDR activati
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Overall the DDR kinase domain has a
2020-10-26
Overall, the DDR1 kinase domain has a typical kinase domain structure and adequate sequence and/or structure similarity with other kinase domains, as shown in Fig. 2, which allow homology modeling of the active and inactive conformations. In addition to conformational changes to the activation loop
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DAPK is a kD Ca
2020-10-26
DAPK is a 160-kD Ca2+/calmodulin (CaM)-regulated Ser/Thr kinase that mediates cell death. The activated forms of DAPK and DRP-1 are capable of inducing two distinct cytoplasmic events characteristic of programmed cell death, including membrane blebbing and the formation of autophagic vesicles (Inbal
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br Conclusion The preclinical data reported
2020-10-26
Conclusion The preclinical data reported in this study shows that LAS191859 is a potent and safe CRTh2 antagonist, with a long receptor residence time that provides a sustained in vivo efficacy. This property is reflected in the prolonged duration of action of LAS191859 in in vitro and in vivo fu
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The present findings suggested that
2020-10-26
The present findings suggested that nsEP inhibited CPG2 via deprivation of zinc ions, with no effect on apoenzyme integrity. Zinc may be removed from CPG2 by the electric forces. Within CPG2, each zinc ion was coordinated by one histidine, one glutamate and one aspartate [6]. The nsEP field can alte
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br Materials and methods br Results br Discussion In
2020-10-26
Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi
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Previous studies demonstrated that cPLA translocates to the
2020-10-23
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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In contrast to inflammatory cytokines TGF has immunosuppress
2020-10-23
In contrast to inflammatory cytokines, TGF-β has immunosuppressive properties yet is also important for tissue imprinting immune cell function during development [23]. Salivary gland (SG) ILCs, in addition to liver and intestinal intraepithelial ILC1, express markers denoting tissue residency and TG
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Transduction of cellular signals by G
2020-10-23
Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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Here we show that cpg is expressed only in
2020-10-23
Here, we show that cpg2 is expressed only in the GKT137831 and encodes a protein that localizes specifically to the postsynaptic endocytic zone of excitatory synapses. We present evidence that CPG2 is a critical component of the postsynaptic endocytic pathway that mediates both constitutive and act
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br Materials and methods br
2020-10-23
Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi
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