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Raloxifene is a second generation SERM that has
2021-03-12

Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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The mechanisms by which Cav enhances embryonal tumor progres
2021-03-12

The mechanisms by which Cav-1 enhances embryonal tumor progression are currently unknown. Given the documented ability of Cav-1 to drive increased biogenesis of caveolae and accelerate the flow of nutrients (mostly glucose and fatty acids) across the membrane, as observed in particular in adipocytes
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br Declaration of conflicting interests br Funding The autho
2021-03-12

Declaration of conflicting interests Funding The author(s) disclosed receipt of the following financial support for the research, authorship, and/or publication of this article: This work was supported by CT Stem Cell grant # 15-RMB-YALE-07 (to L.E.N), and by an unrestricted Research Gift from
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Although MMP might be a downstream target of
2021-03-12

Although MMP-9 might be a downstream target of Src kinase signaling (Liu and Sharp, 2011), a direct connection has not been established. We showed for the first time that, in the collagenase-induced ICH model, Src kinase signaling regulates MMP-9 activity and mediates EP1R toxicity. Consistent with
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Enzyme activity loss during the
2021-03-12

Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important
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br Oxidoreductase like MEM for prodrug
2021-03-12

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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br ET Antagonist for the
2021-03-12

ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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Despite the significant increase in Bdnf mRNA levels after
2021-03-12

Despite the significant increase in Bdnf1 mRNA levels after DNMT inhibition, the expression of Bdnf4 and Bdnf9 was unaltered. It is particularly surprising that Bdnf4 is not affected by the DNMT inhibitor, as the promoter of the Bdnf4 exon is known to be susceptible to epigenetic changes (Kotera et
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Chemokines act as ligands for the chemokine receptors which
2021-03-11

Chemokines act as ligands for the chemokine receptors, which possess 7-transmembran domain-type proteins functionally coupled to G proteins. Leukocytes express 19 chemokine receptors which control their influx and activation at the site of inflammation. Human neutrophils express both CXCR-1 and CXCR
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Given a disruption of membrane internalization and an increa
2021-03-11

Given a disruption of membrane internalization and an increase in synaptic glutamate receptors in CPG2 knockdown neurons, one might expect an increase in dendritic spine size as membrane continues to be inserted into the spines during receptor exocytosis. However, we observed the opposite phenotype,
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Recent studies showed that the
2021-03-11

Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-
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br Method Detailed study protocol was reported
2021-03-11

Method Detailed study protocol was reported previously. The ULTIMATE- HFrEF trial was approved by the Institutional Review Board of our hospital, and the study drug, udenafil, was approved as Investigational New Drug for treatment in patients with chronic HFrEF by Ministry of Food and Drug Safety
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In mammals ribonucleotide reductase RNR is a unique
2021-03-11

In mammals, ribonucleotide reductase (RNR) is a unique enzyme that catalyzes the rate-limiting step of de novo synthesis of deoxyribonucleoside triphosphates (dNTPs).7, 8 Mammalian RNR consists of two homodimer subunits: the large catalytic dimer RRM1 and the small regulatory dimer RRM2 or RRM2B. An
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Importantly our in vivo data fit to the in
2021-03-11

Importantly, our in vivo data fit to the in vitro data, further confirming the synergistic effect of XJD and gefitinib on the inhibition of lung cancer and the regulation of SP1, HOTAIR, and EP4 iwp2 levels. The doses of XJD used were based on our previous in vivo study (Zhao et al., 2016). We beli
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The eNOS bp VNTR polymorphism has
2021-03-11

The eNOS 27-bp VNTR polymorphism has been found to be associated with altered plasma NO levels. This polymorphism also has been associated with many vascular diseases including hypertension, diabetic retinopathy, and diabetic nephropathy in various populations. Notably, our results were different fr
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