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As proof of principle the effect of selective blockade was
2020-09-21
As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration
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During the entire life of
2020-09-21
During the entire life of individual, articular chondrocyte as well as subchondral bone receives acute or chronic stress. Joints homeostasis is maintained by biomechanical stress, as rapid loss of proteoglycan in joints occurs due to immobilization or disuse. These osteophytes are fibrocartilage cap
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Like compound substitution on compound contains
2020-09-21
Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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The aniline R group was extensively explored
2020-09-21
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Merimepodib In this study EDC NHS crosslinked collagen films
2020-09-21
In this study, EDC/NHS crosslinked collagen films were derivatised with VWFIIINle-containing THPs and the effect on VWF and DDR2 activity was examined. First, we investigated restoration of the binding of DDR2 and VWF A3. Cell behavior beyond simple binding was also investigated through DDR2 Merimep
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Interestingly some drugs have been shown to
2020-09-21
Interestingly, some drugs have been shown to be effective in the regulation of cytokine production (such as IL-2, IL-10, IL-27, IL-35, IL-37 and transforming growth factor-β, TGF-β) and, therefore, having a key role in the management of certain inflammatory-based clinical conditions (Banchereau et a
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The first transcription factor TF known to
2020-09-21
The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone BI 6015 of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed development an
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The heterogeneity among studies that investigated
2020-09-19
The heterogeneity among studies that investigated the association of COMT Val158Met with alexithymia was also significant (Ham et al., 2005; Min et al., 2016; Swart et al., 2011; Zekioglu et al., 2014). The healthy status, drug effect, and other demographic variables also influenced one\'s ability o
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There are studies that evaluated the stability of CMV
2020-09-19
There are studies that evaluated the stability of CMV DNA over different periods of time. A study that evaluated stability of EDTA plasma samples stored over a 21-day period at 4 °C found no significant change in the viral loads or any trend of continued DNA degradation [9]. Another study did not fi
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IAA sensitive Cl channels were
2020-09-19
IAA-94-sensitive Cl channels were shown to mediate cardioprotection due to IPC (Diaz et al., 1999) and cyclosporine A (Diaz et al., 2013). CLIC-like channel activity was also observed in cardiac mitoplast (Misak et al., 2013) but the molecular identity of these intracellular Cl channels and their pr
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It is well known that Doxorubicin induced cardiotoxicity occ
2020-09-19
It is well known that Doxorubicin-induced cardiotoxicity occurs via p53-mediated apoptosis (Lorusso et al., 2007). However, there are few studies elucidating the mechanism of HFS induced by PLD. We found that PLD induces keratinocyte apoptosis in a very low dose, and the damage induced by PLD cannot
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Oxidative stress is associated with elevated levels of intra
2020-09-19
Oxidative stress is associated with elevated levels of intracellular reactive oxygen species (ROS) generation which then causes DNA damage and the death of cells (Miyata et al., 2017). Generation of ROS affects main signaling pathways in cells associated with tumorigenesis: mitogen activated protein
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Arsenic is an endocrine disruptor with estrogenic activity
2020-09-19
Arsenic is an endocrine disruptor with estrogenic activity. Further study has shown that arsenic exposure can significantly increase the expression of estrogen receptor-related genes, steroid metabolism-related enzymes and lung cancer-related genes in the lung tissues of female mice on the occurrenc
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In humans the ER is
2020-09-19
In humans, the ERα is encoded by the gene ESR1, located on chromosome 6, locus 6q25.1 (Gosden, Middleton, & Rout, 1986). In addition to the full-length ERα isoform (66kDa), several shorter isoforms (36kDa, 46kDa) have been identified as a result of the presence of alternate start codons, or as produ
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Our previous studies have shown that in a preimplantation mo
2020-09-19
Our previous studies have shown that in a preimplantation mouse embryo the proportion of inner to outer cells (i.e. precursors of ICM and TE, respectively) is regulated by a different frequency of differentiative cell divisions at the 8- and 16-cell stages. Low number of inner blastomeres generated
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