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The optimization of the lead compound was
2020-11-02

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 sanguinarine moiety with other functional groups led to loss of functional activity against EP4 receptor
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To identify and characterize new possible molecular targets
2020-11-02

To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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Introduction Protein ubiquitination is a posttranslational
2020-10-31

Introduction Protein ubiquitination is a posttranslational modification that plays a major role in almost all cellular processes in eukaryotes (Hochstrasser, 2009; Komander & Rape, 2012). It involves the covalent attachment of ubiquitin (Ub) via its C-terminal glycine carboxylate to a primary amine
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br Experimental methods br Results and discussion br Conclus
2020-10-31

Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.
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Previous studies showed that many
2020-10-31

Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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Abrahamson and coworkers recently demonstrated a distinct
2020-10-31

Abrahamson and coworkers (2009) recently demonstrated a distinct role of the podocyte in preservation and production of mature GBM-components such as α3/4/5(IV)-chains. This group further verified that collagen receptors (integrins) are linked to the DS2 of podocytes. In accordance to this data, ou
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Almost of drugs in the
2020-10-31

Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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Data from our in vitro studies using BEAS B cells
2020-10-31

Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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Unlike many forms of SNHL cCMV may
2020-10-31

Unlike many forms of SNHL, cCMV may be treatable. The antiviral drug valganciclovir (VGCV) has been proposed to improve hearing, speech, and language outcomes associated with this infection [6]. A recent publication from the CASG (Collaborative Antiviral Study Group) reported that a six-month course
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br Acetylcholinesterase and cholinergic signaling
2020-10-31

Acetylcholinesterase and cholinergic signaling The concept of a synapse between a neuron and an innervated cell, and the receptors that mediated their interaction, was developed by Bernard, Ehrlich, Sherrington, Langley and others (see [7], [8], [9]. It was long debated whether transmission of ne
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In contrast to drospirenone dydrogestrone acts rather neutra
2020-10-31

In aldose reductase to drospirenone dydrogestrone acts rather neutral at the aldosterone-, glucocorticoid- and androgen-receptor [12]. This indicates that the assessment of a ‘net-overall effect’ on the vascular system is very difficult based on the often discussed ‘partial effects’ of the progesto
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PGE EP activation has been found to attenuate the
2020-10-31

PGE2-EP4 activation has been found to attenuate the activation of microglia and to prevent lipid peroxidation and pro-inflammatory gene expression in a murine model of lipopolysaccharide (LPS)-induced crf1 inflammation [15]. Moreover, PGE2/EP4 signaling has elicited a protective function in reducin
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Introduction PGE is a major mediator present
2020-10-31

Introduction PGE2 is a major mediator present at sites of inflammation [1]. It is well established that PGE2 contributes to the localized and systemic symptoms of inflammation. A key study by Portanova et al. [2] demonstrated that anti-PGE2 cmv virus were able to reverse the swelling and pain in lo
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TgTCEA from petals TgTCEA and
2020-10-31

TgTCEA from petals (TgTCEA1) and TgTCEB from pollen grains (TgTCEB1) were used throughout the study. The recombinant enzymes were expressed in , and purified as the His-tag-free forms as described previously., Enzyme reactions were performed at 4 mM substrates under the same conditions as described
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Inappropriate heme metabolism has been linked to several neu
2020-10-31

Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer\'s disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 2
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