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For the current studies we used
2020-06-09
For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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In summary EP signaling modulates heteromeric kainate recept
2020-06-09
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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Binding affinity was measured by a scintillation proximity
2020-06-08
Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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On the opposite side sPLA X has also been implicated
2020-06-08
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer IFN-alpha 1, human recombinant protein synthesis and promotes their survival during nutrient stress. It a
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br Materials and methods br Results
2020-06-08
Materials and methods Results Discussion Although some conditioning therapies have provided satisfactory clinical outcomes, mammalian species have little or no ability to replace injured cardiac tissue [34]. Therefore, therapeutic strategies based on the prevention, rather than treatment af
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br Acknowledgments We thank our colleagues who
2020-06-08
Acknowledgments We thank our colleagues who have contributed to our understanding of the N-3-oxo-dodecanoyl-L-Homoserine lactone and the structure and function of APC/C, and apologize to those whose work we were unable to cite here. We thank J. Rajan Prabu for making the movies showing APC/C con
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DNA PK Jackson is activated by
2020-06-08
DNA-PK (Jackson, 1997) is activated by DNA double-stranded breaks (DSBs). It is a trimeric complex composed of the catalytic subunit, DNA-PKcs, and the Ku70/80 heterodimer. DNA-PK mediates non-homologous end joining (NHEJ), which joins programmed DSBs created during V(D)J recombination and class swi
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Pleuromutilin sale High throughput screening HTS of the
2020-06-08
High throughput screening (HTS) of the AstraZeneca Pleuromutilin sale collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM
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br Type II NAD P H Dehydrogenases
2020-06-08
Type II NAD(P)H Dehydrogenases in Fungi Fermentative YeastSaccharomyces cerevisiaeBecause S. cerevisiae is a facultative 1027 receptor yeast capable of meeting its energy requirements with ATP generated by fermentation, only relatively few mitochondrial proteins are essential for cell viability.
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Our data show a site specific interaction of DDR
2020-06-08
Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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Consistent with previous simulations on the
2020-06-08
Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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The anxiolytic like responses produced by
2020-06-08
The anxiolytic-like responses produced by anti-SVG-30 suggests that CRF2 receptors mediate not only the elicitation of anxiety behavior induced by prior stress, i.e. conditioned freezing, but also unconditioned anxiety behavior induced by exposure to the unfamiliar environment of the elevated plus m
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-06-08
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead BAPTA-AM synthesis 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other
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Although many neurotransmitters e g catecholamines serotonin
2020-06-08
Although many neurotransmitters (e.g., catecholamines, serotonin, and excitatory/inhibitory amino acids) have been implicated in the modulation of anxiety-like responses (Carobrez et al., 2001, Molchanov and Guimaraes, 2002, Vianna et al., 2001), the so-called atypical neurotransmitters, endocannabi
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The performance of the qCPA approaches is similar with
2020-06-08
The performance of the qCPA approaches is similar with regards to the derivative properties of CO2 and for mixtures of CO2+self-associating compounds. For CO2+n-alkanes the four-parameter versions of qCPA both perform somewhat better than the three-parameter version. Nevertheless this modest improve
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