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CaneCPI showed strong inhibitory activity against recombinan
2021-07-02
CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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Some studies have demonstrated that BMSCs can provide severa
2021-07-02
Some studies have demonstrated that BMSCs can provide several trophic and growth factors that play important roles in cell survival, angiogenesis, and BMSC differentiation, but not cell replacement (Peled et al., 1999, Shen et al., 2007, Ji et al., 2004). This paracrine effect of BMSCs is a potentia
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Previously we had proposed three possible
2021-07-02
Previously we had proposed three possible models, with one being that hCrm1 fundamentally interacted more favorably or strongly with Rev-RRE complex, compared to mCrm1. We decided to test that model, which was the simplest and most straightforward, by both biochemical and genetic means. By using bac
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Besides the assessment of toxicological effects immediately
2021-07-02
Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c
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We further analyzed the transcriptional mechanisms underlyin
2021-07-02
We further analyzed the transcriptional mechanisms underlying the synergistic action of IL-23 and PGE2 and found that this action is mediated by not only STAT3 but also CREB1 and NF-κB. Involvement of CREB1 is analogous to that in the PGE2-EP2/EP4–mediated Il12rb2 induction during TH1 cell different
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The optimization of the lead
2021-07-02
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Pyrene azide 3 moiety with other functional groups led to loss of functional activity against EP4 receptor
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In summary EP signaling modulates heteromeric
2021-07-02
In summary, EP1 signaling modulates heteromeric kainate receptors at multiple steps, both sensitizing mice to kainate-evoked status epilepticus and, separately, exacerbating the downstream consequences of status epilepticus. These results, together with those of Serrano et al. (2011) and Jiang et al
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br Activatable bioorthogonal reactions reagents br
2021-07-02
Activatable bioorthogonal reactions/reagents Cyclopropenes as bioorthogonal reagents for IEDDA substrates Cyclopropenes have become popular bioorthogonal reagents due to their small size, inertness to biological nucleophiles, ability to be genetically encoded (Yu et al., 2012), and participati
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Another enzyme class that has emerged
2021-07-02
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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In order to derive a better understanding of the
2021-06-29
In order to derive a better understanding of the results from our SAR study, we utilized Glide to model the binding of the SAR compounds with the non-active site pocket of TS-DHFR shown in C. The majority of models position the phenolic moiety of these compounds within the non-active site pocket, wh
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Several of the keloid like lesions
2021-06-29
Several of the keloid-like lesions seen in these individuals were pigmented. It is of potential relevance that genetic variants in DDR1 [MIM: 600408] have been associated with vitiligo, and DDR1 activation is involved when triclosan products receptor are attached to collagen-IV fibers. Because DDR1
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It is now widely known that blockade of
2021-06-29
It is now widely known that blockade of CysLT1 receptors strongly inhibits antigen-induced bronchial contractions in specimens isolated from non-asthma subjects. However, this blockade is not complete as shown in the present study and in other literature.4, 15, 16 The results of the current study su
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Tirapazamine In conclusion we developed a new CysLT and
2021-06-29
In conclusion, we developed a new CysLT1 and CysLT2 receptors-mediated anaphylaxis guinea pig model that can be useful for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. In addition, we have shown that the dual CysLT1/2 receptor antagonist ONO-6950 can exert protective effect aga
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Yang et al investigatedPsoralidin a coumestan derivative iso
2021-06-29
Yang et al. investigatedPsoralidin 39, a coumestan derivative isolated from the seed of Psoralea corylifolia, regarding its effects on IR-induced pulmonary inflammation. Psoralidin 39 inhibited the IR-induced COX- 2 expression and PGE(2) production through regulation of PI3K/Akt and NF-κB pathway.
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Coumarins also known as benzopyran
2021-06-29
Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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