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A novel series of DHODH
2021-06-04
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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The aberrant methylation of genes that suppress tumorigenesi
2021-06-04
The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr
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During host cell interactions G intestinalis trophozoites up
2021-06-04
During host-cell interactions, G. intestinalis trophozoites up-regulate several cell-associated proteins, including high-cysteine membrane proteins (HCMPs) and variant surface proteins (VSPs) [8]. The parasite also releases around 200 proteins upon host-cell contact, including many proteases [9,10].
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By using the C elegans Matrisome Annotator tool we found
2021-06-03
By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome Phenyl sulfate in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elegans matrisome for
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br Halogenases Enzymatic C H activation leading to
2021-06-03
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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Bedaquiline The aim of this paper is to study the
2021-06-03
The aim of this paper is to study the long-term socioeconomic impacts of local heat entrepreneurship from 2000 to 2016. The analysis focuses on impacts of the biomass-based district heat production on employment and income in a small peripheral community, called Eno, located in North Karelia, Finlan
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Dual inhibition of ACE and NEP as a strategy
2021-06-03
Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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The different serotypes A G have unique receptors to which
2021-06-03
The different serotypes (A-G) have unique receptors to which they bind to produce the toxic effect on the nerve cells. (Lance, 2004, Rosetto et al., 2014). Intracellularly, the endopeptidase activity of different serotypes of BoNT target selectively a unique group of proteins, the SNARE 1295 sale (K
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Itch also known as astrophin interacting protein AIP is a
2021-06-03
Itch, also known as astrophin-1 interacting protein-4 (AIP4), is a HECT domain-E3 ligase. It was discovered in 1998 in mouse coat color genetic studies which displayed the disruption caused by the Itch gene inducing a lethal autoimmune inflammatory condition. The substrates of Itch are transmembrane
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Because of the important role of the DDB
2021-06-03
Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup
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Advances in the total chemical
2021-06-03
Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio
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The expression of cytokine inducible genes is mediated
2021-06-03
The expression of cytokine-inducible genes is mediated by a number of components within the cell. It has been shown that Jak2 and the Ras/Raf/MAP kinase signaling cascades are required for the expression of DUB-1[9], [29]. However, the enhancer domain of DUB-1 lacks a consensus sequence for Stat bin
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br Introduction Type Diabetes mellitus T DM is a
2021-06-03
Introduction Type 2 Diabetes mellitus (T2DM) is a metabolic disorder that raises blood glucose level for a prolonged time. T2DM is associated with acute complications like ketoacidosis, hyposmolar coma, chronic complications include heart disease, stroke, kidney failure, foot ulcers and damage to
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br Development of the double strand break repair
2021-06-03
Development of the double strand break repair model for meiotic recombination Meiotic recombination was first described by Frans Alfons Janssens using Ozagrel in the salamander Batracoseps attenuatus in 1909 [21] and then further elaborated at the genetic level in Drosophila by Thomas H. Morgan [
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In summary the loss of seven Cyp a genes lead
2021-06-02
In summary, the loss of seven Cyp3a genes lead to sexual dimorphic changes during the eight weeks of high fat diet treatment with Cyp3a-null female mice showing a healthier acclimation to a high fat diet through decreased weight gain, higher adiponectin, lower B-OHB levels, and a better response to
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