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623 Here we describe a novel series
2021-04-30

Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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CRF and urocortin produce marked effects on
2021-04-30

CRF and urocortin 1 produce marked effects on the CPI-455 when administered both i.v. or directly into the CNS (Parkes et al., 2001). Systemic i.v administration of CRF and urocortin 1 cause a marked and long-lasting reduction in mean arterial blood pressure in rats Briscoe et al., 2000, Lawrence e
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br Results and discussion br Conclusion br Experimental
2021-04-30

Results and discussion Conclusion Experimental section Pharmacological studies Introduction Survival analysis is a set of statistical methods that aim at modeling the relationship between a set of predictor variables and an outcome variable and, in particular, prediction of the time w
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Social memory is encoded within certain sites but meaning de
2021-04-30

Social memory is encoded within certain sites, but meaning depends upon an interpretant (such as a tourist) being able to decode the signs. Memorials, such as cemeteries, require some kind of activity by its visitors for their meanings to be activated (Hutchinson, 2009, Winter, 2010). Following Eden
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br Introduction Breast cancer is the
2021-04-29

Introduction Breast cancer is the most common cancer in women and one of the leading causes of death worldwide. Estrogen receptor alpha (ERα, “wild-type” estrogen receptor), encoded by the estrogen receptor1 (ESR1) gene, is expressed in approximately 70% of all breast cancers. Hormonal therapy ha
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Our results demonstrated that ET a Wnt
2021-04-29

Our results demonstrated that ET-1, a Wnt ligand, stimulated the Wnt/β-catenin signaling pathway. First, ET-1/ETRA binds to Frizzled family cell-surface receptors, resulting in the activation of Dvl1, a Dishevelled (DSH) family protein. Next, activated DSH inhibits the Axin, GSK-3β, and APC protein
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Two GPCR subtypes of interest in the myocardium are
2021-04-29

Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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Polymorphism of the CD gene
2021-04-29

Polymorphism of the CD226 gene also affected the progression rate without any significant effect on autoantibody formation. This gene has been reported to be a common genetic factor in multiple autoimmune diseases such as SLE, systemic sclerosis and type 1 diabetes [43]. CD226 is an immunoglobulin s
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Currently much effort has been made to
2021-04-29

Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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br Regulation of DGK activity
2021-04-29

Regulation of DGK activity Activation of the DGKs is complex and unique for each DGK isotype. In most cases, DGKs must translocate to a membrane compartment to access DAG. However, translocation does not necessarily activate the enzyme [57]. In addition, DGK activity can be modified by other cofa
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There is literature precedence for
2021-04-29

There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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In a recent study Tomkins et
2021-04-29

In a recent study, Tomkins et al. [7] analyzed the protein-protein interaction network of ROCO proteins. Based on a database analysis, and only taking into account interactions reported in at least two peer-reviewed papers and/or confirmed by two different methods, 113 interactors were revealed for
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Currently it is not known if
2021-04-29

Currently, it is not known if drought induces changes in the cysteine protease n-acetyl-l-cysteine of soybean nodules. The available annotation of the soybean genome, in Phytozome (www.phytozome.net) has identified 706 C1 cysteine protease sequences and 75 C13 cysteine proteases. We have previously
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Experiments on the rat model of E
2021-04-29

Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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Previously to detect CDKL activity we
2021-04-29

Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti
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