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Instead of receptor interaction or
2019-07-02
Instead of receptor interaction or GT activity, we focused on the CPD and autoprocessing. The CPDs from the 2 toxins are highly homologous: each cysteine protease targets an intramolecular substrate and mediates InsP6-induced autoprocessing to release the GTD into host cytosol.40, 41 However, TcdB i
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Cysteine protease inhibitors representing several chemical s
2019-07-02
Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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br Introduction The allergic response
2019-07-02
Introduction The allergic response is a complex process involving the interaction of several mediators; among these, cysteinyl leukotrienes (CysLTs) represent one of the most important actors in the pathogenesis of airway allergic diseases such as allergic rhinitis and asthma [1]. Pharmacological
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CEP-37440 CK comprises a family of
2019-07-02
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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EBI and its ligand s EBI was found in
2019-07-02
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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With a favorable spectrum of CRTh
2019-07-02
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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Apart from neutrophil mediated inflammation
2019-07-02
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α prod
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br Materials and methods br Results
2019-07-02
Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration ha
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Different types of environmentally induced
2019-07-02
Different types of environmentally induced antinociception have been reported in a wide range of species (e.g., Behbehani, 1995, Bolles and Fanselow, 1980, Harris, 1996, Millan, 2002, Rodgers, 1995). According to Bolles and Fanselow (1980), fear and pain are independent and competing motivational sy
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In this study we observed alterations
2019-07-02
In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased L-α-Aminoadipic Acid when the sensitization condition was established. Similarly, CRF2 rece
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Here we show that cpg is expressed
2019-07-02
Here, we show that cpg2 is expressed only in the Puromycin 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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Additionally both in vitro and
2019-07-02
Additionally, both in vitro and in vivo studies showed that a Ca2+ influx is closely related to apoptosis (Rizzuto et al., 2003). Calmodulin (CaM) is a multifunctional intermediate calcium-binding messenger protein expressed in all eukaryotic cells, which senses intracellular calcium levels by bindi
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In conclusion the data suggest that doses
2019-07-02
In conclusion, the data suggest that doses of COX-2 inhibitors and EP1 receptor antagonists which have previously been reported to exert disease modulating or antiepileptic drug potentiating effects do not negatively affect seizure control in temporal lobe epilepsy. The contrasting impact of the EP1
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Repulsive interactions towards undesirable substrates
2019-07-02
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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What are the molecular signals that guide Tfh cells
2019-07-02
What are the molecular signals that guide Tfh cells as they navigate around the lymph node in the course of the immune response? It was recently reported that Tfh cells inside GCs have high expression of SIPR2, which acts to repel them from the S1P-rich lymph in the SCS and promote their retention i
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