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With a favorable spectrum of
2020-05-08
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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We have previously characterized the leucine rich
2020-05-08
We have previously characterized the leucine-rich NESs located within the zinc-binding domains of mucosal high risk HPV16 E7 (76IRTLEDLLM84) and low risk HPV11 E7 (76IRQLQDLLL84) mediating their nuclear export in a CRM1 dependent manner (Knapp et al., 2009, McKee et al., 2013). The zinc-binding doma
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The crystal structure of LiCoO is presented in Fig We
2020-05-08
The crystal structure of LiCoO2 is presented in Fig. 1. We can notice that the Li and Co atoms occupy the centers of two different edge-sharing [CoO6]-octahedra, which results in formation of separate Li and Co layers. Hence, the layered structure of LiMO2 is able to intercalate lithium into transit
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This paper proposes an acceptance
2020-05-08
This paper proposes an acceptance process and evaluation criteria, specialized for the dedication of indirect COTS SW as well as direct ones. (Step 1) It first recognizes an indirect COTS SW as a target of dedication, unlike EPRI NP-5652/TR-106439. (Step 2) It then determines the safety category of
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SCR7 Measurement of Chol absorption synthesis and catabolism
2020-05-08
Measurement of Chol absorption, synthesis and catabolism would be very helpful to determine the underlying cause of hypercholesterolemia in individual patients at risk for atherosclerosis. The information could help to determine the best therapeutic approach to reduce Chol absorption, to reduce Chol
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br Effects of estrogens on bone Estrogens
2020-05-08
Effects of estrogens on bone Estrogens play an important role in bone remodeling, as demonstrated by studies in mice in which the ER genes were deleted [21], [22]. ERβ compensates for the HJC 0350 of ERα, and vice versa, but when both ERs are deleted a profound decrease in trabecular bone volume
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br Conformational properties of DGK br
2020-05-07
Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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Experimentally measured DGAT activity was first reported by
2020-05-07
Experimentally measured DGAT activity was first reported by Weiss et al. (1960) and several different types of DGAT enzyme have since been described in plants [12,41,42]. As recently as 2011 there appeared to be just two DGAT enzymes both in plants and in other eukaryotes, namely DGAT1 and DGAT2 [43
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br The DDR kinase domain The
2020-05-07
The DDR1 kinase domain The DDR1 intracellular kinase domain shares the typical structure of other kinase domains (Fig. 1). However, how DDR1 kinase is activated upon collagen binding is poorly understood. It is thought that the process is fundamentally different from the accepted paradigm of liga
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In order to gain further insights into
2020-05-07
In order to gain further insights into the role of peptidases in B. xylophilus, four cysteine proteases highly secreted by B. xylophilus (Cardoso et al., 2016) were selected four further characterisation. Materials and methods Results and discussion Structural prediction and analysis The i
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We hypothesized that the atopic phenotype may be partially
2020-05-07
We hypothesized that the atopic phenotype may be partially influenced by an altered binding and/or signalling due to the amino-acid substitution in the receptor protein. The principal aim of this study was to investigate the signalling mechanisms of the variants CysLT1-G300S and CysLT1-I206S induced
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The consistent anti anxiety effects obtained with intra
2020-05-07
The consistent anti-anxiety effects obtained with intra-mPFC injections of CP 376395 strongly suggest a tonic role of CRF at CRF1 receptors located within this limbic PF 4800567 hydrochloride synthesis area in the modulation of anxiety in the mouse on the EPM. Intra-mPFC injection of CP 376395 led
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Carnitine acetyltransferase CrAT transesterifies short chain
2020-05-07
Carnitine acetyltransferase (CrAT) transesterifies short-chain acyl-CoAs, and is located both in mitochondria and peroxisomes. In yeasts and mammals this protein is the product of a single gene [20,21] and the sorting to different organelles is evolutionary conserved, although the mechanism of diffe
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Recent studies showed that the
2020-05-07
Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-
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Hymenialdisine the most potent inhibitor of parasite TgCK en
2020-05-07
Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this T16Ainh - A01 also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of C
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