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pd184352 receptor Xenobiotic metabolism primarily occurs in
2020-08-10
Xenobiotic metabolism primarily occurs in liver, which contains many enzymes to catalyze the transformation of xenobiotic. Usually, cytochrome P-450s (CYP450s) act as the first response for biotransformation of xenobiotic in organisms. CYP450s generally consist of various subfamily enzymes which can
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Eukaryotic cell cycle machinery is thought to appropriately
2020-08-10
Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me
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An increased CK activity was
2020-08-10
An increased CK2 activity was found in septal neuronal 15-deoxy-Δ-12,14-Prostaglandin J2 australia dissected from rat embryos after hypoglycemia [36]. These data indicated that CK2 activity is not only regulated by insulin but also by the glucose concentration. One essential step in insulin action
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We showed for the first time that ivermectin significantly
2020-08-10
We showed for the first time that ivermectin significantly reduced the pH-induced response of the pHCl-A variant at 300nM, whereas fipronil and γ-BHC had no significant effects on the channel unlike in RDL and GluCl (Fig. 4). Such a concentration is similar to the threshold at which ivermectin activ
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An important focus of the
2020-08-10
An important focus of the present study has been the interaction of HUVECs with extracellular matrix in the regulation of angiogenesis. Matrigel is a gelatinous protein extract secreted by Engelbreth–Holm–Swarm mouse sarcoma cells, and is considered to be a good model of the extracellular matrix (Kl
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We next turned our attention to the position
2020-08-10
We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional ass
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br Oxidoreductase like MEM for prodrug activation br Future
2020-08-10
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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To provide a brief critical evaluation of this technology an
2020-08-10
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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The elastase induced injury model has
2020-08-10
The elastase-induced injury model has been shown to produce airspace enlargement, and increases in lung volume and compliance that are similar to those observed in human patients (Hantos et al., 2008, Hamakawa et al., 2011). Thus, this model, which has been used to study emphysema, should be adequat
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br Introduction Esophageal squamous cell carcinoma ESCC
2020-08-10
Introduction Esophageal squamous cell carcinoma (ESCC) is one of the most common types of cancer in East Asia and is a leading cause of cancer-related death worldwide.1, 2 Surgery is widely used for treatment in localized disease, where it can provide definitive management and potential cure. Tre
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TC-I 15 While oxysterols were most extensively
2020-08-10
While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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Covalent inhibitors are well suited for targeting
2020-08-09
Covalent inhibitors are well suited for targeting the E1 Deferiprone of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in cir
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br Conflicts of interest br Introduction G protein coupled r
2020-08-09
Conflicts of interest Introduction G protein-coupled receptors (GPCRs), form the largest human membrane protein family, with 800 members overall. Many druggable targets for treatment of common diseases involve GPCRs that mediate therapeutic effects of 34% of all marketed drugs (Hauser, Attwood
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br Results To understand how
2020-08-08
Results To understand how Rad53 functions to maintain replisome integrity, we first analyzed newly synthesized leading- and lagging-strand DNA in wild-type (WT) and rad53-1 mutant cells using BrdU-IP-ssSeq, a method that detects synthesis of both leading and lagging strands (Yu et al., 2014). Bri
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Because of the complexity of DNA damage and
2020-08-08
Because of the complexity of DNA damage and its repair, several pathways are candidates in HN2-induced DPC repair. Considering the 23kDa molecular weight of MGMT, NER may be ineffective for MGMT-adduct removal. This presumption is supported by that the mRNA level of ERCC1, a core gene in NER pathway
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