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In conclusion we designed novel E inhibitors based on the
2020-02-11
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,
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Several studies highlighted the potential of EOCs
2020-02-11
Several studies highlighted the potential of EOCs to promote adverse effects on aquatic organisms. It was reported the toxicity of BPA to invertebrates and fish, and the effect of lipophilicity on toxicity was analyzed (Mathieu-Denoncourt et al., 2016). There was reported the effects of PPCPs on aqu
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M 1145 br Expression data suggest involvement
2020-02-11
Expression data suggest involvement of additional TRIMs in heart function Given the complexity of the cardiac function, involved molecular pathways and processes, and the fact that only a few of the TRIMs have thus far been shown to have a cardiac role, we hypothesized that there would be more TR
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Preliminary studies evidenced the presence
2020-02-10
Preliminary studies evidenced the presence of CRFr in gamma-aminobutyric acid-ergic (GABAergic) neurons of the hippocampus (Yan et al., 1998). In fact, in this ccr2 inhibitor area, CRF inhibits glutamate release through CRF1r (Bagosi et al., 2015), leading to a decrease in the GABA concentration in
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br Funding sources br Introduction Psychiatric comorbidities
2020-02-10
Funding sources Introduction Psychiatric comorbidities affect up to 70% of people with pharmacoresistant epilepsy and significantly impact quality of life [1]. Psychiatric comorbidities in epilepsy have been thought to be due to psychosocial stress. However, recent evidence suggests a more com
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The mitogen activated protein kinase MAPK family which consi
2020-02-10
The mitogen-activated protein kinase (MAPK) family, which consists of extracellular signal-regulated protein kinase 1/2 (ERK1/2), p38 MAPK, and c-Jun N-terminal kinase (JNK), is involved in the development of NP (Hung et al., 2012, Ji et al., 2009). Recently, Zhuang et al. (2005) demonstrated that t
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EPAC activation in VSMCs and ECs reverses several processes
2020-02-10
EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show
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br Orthotopic liver transplantation OLT is the only curative
2020-02-10
Orthotopic liver transplantation (OLT) is the only curative therapy available for patients with end-stage liver disease. The surgical procedure of liver transplantation inherently involves cold ischemia during graft preservation , followed by reperfusion of the transplanted graft which results in
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GPR also known as EBI is a G
2020-02-10
GPR183 (also known as EBI2) is a Gαi-coupled seven-transmembrane chemotactic receptor. It is highly expressed on follicular B cells, CD4+ dendritic cells (DCs), and CD4+ T cells but is downregulated on germinal center (GC) j 14 synthesis in secondary lymphoid organs and controls cell migration to a
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br Conclusion From the series of synthesized N methylated an
2020-02-10
Conclusion From the series of synthesized N-methylated and N-benzylated pyrimidinediones, it may be concluded that the presence of electron rich species with pyrimidinediones is vital for enhancing binding with target, although, incorporation of steric bulky group must be taken into consideration
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Predictions of enzyme topology for DGAT are
2020-02-10
Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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br Materials and methods br Results br Discussion
2020-02-10
Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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br Materials and methods br Results br Discussion
2020-02-10
Materials and methods Results Discussion In the present study, as a trial to evaluate the marine ciliate E. crassus for further studies, its susceptibilities to B[a]P and β-NF were measured. Acute toxicity of B[a]P in aquatic organisms has been extensively studied, but not enough data is av
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A topological property P is said to
2020-02-08
A topological property P is said to be cut point hereditary [3] if whenever a space X has property P, then, for every there exists some separation of such that each of and has property P. A space X is called connected ordered topological space (COTS) [5] if it is connected and has the property
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The mechanisms by which coregulators
2020-02-08
The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,
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