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In the preclinical evaluation of CRF receptor antagonists ef
2019-11-16

In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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Importantly a crucial role of transcription factor SP in
2019-11-16

Importantly, a crucial role of transcription factor SP1 in mediating the anti-lung cancer effect of XJD was found in this study. Our results suggested that the inhibition of SP1 was required to mediate the inhibitory effect of XJD on the growth of NSCLC cells. Nuclear transcription factors SP1 is as
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The murine subfamily members including and
2019-11-16

The murine subfamily members including , , , and have been identified and their encoded proteins showed deubiquitinating enzymatic activity , , , . It has been demonstrated that is an immediate-early gene induced by IL-3 in B-lymphocytes and is an IL-2 specific immediate-early gene in T-lymphoc
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There have been two reports of tumor shrinkage
2019-11-16

There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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At one time the biological effects of cAMP
2019-11-16

At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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Both receptors belong to the large family of
2019-11-16

Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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GF 109203X Nimodipine administration also inhibited the eIF
2019-11-16

Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s
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RCT pathway plays a critical
2019-11-16

RCT pathway plays a critical role in the maintenance of cholesterol homeostasis by facilitating the cholesterol clearance and cholesterol efflux (Levinson & Wagner, 2015). In the process of RCT, ABCA1 and ABCG1 played as crucial regulators in cholesterol efflux (Yasuda et al., 2011). Compared with h
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All of the studies referred to above
2019-11-16

All of the studies referred to above were on microvillous membrane from hSTB; however, there is little information regarding conductances in the basal membrane. Illsley and Sellers, using a fluorescent technique, determined the relative permeabilities of cations and chloride in basal membrane vesic
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Evidence for interactions between the endothelin and the ang
2019-11-16

Evidence for interactions between the endothelin and the angiotensin system has also become plentiful. It has become clear that the two systems, in addition to acting independently, can act synergistically (Emori et al., 1989, Imai et al., 1992) as well as promote the peptide mRNA expression in endo
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br DDR in atherosclerosis and
2019-11-15

DDR1 in atherosclerosis and vascular disease The Canadian group of Bendeck, explored the role of DDR1 in repair following arterial injury in rats [30]. DDR1 protein levels, assessed via Western blots prepared from arterial extracts taken at various times after injury, showed DDR1 protein dramatic
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KN-93 Phosphate Previous studies from our laboratory in CD m
2019-11-15

Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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The most important cytotoxic lesion formed by the nitrogen
2019-11-15

The most important cytotoxic lesion formed by the nitrogen mustards is generally considered to be the DNA–DNA interstrand cross-link 12, 13. DNA–DNA interstrand cross-links are thought to exert their cytotoxic effects by inhibiting DNA duplex strand separation, progression of the GDC-0084 fork and
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br Acknowledgments This research was financially supported
2019-11-15

Acknowledgments This research was financially supported by National Natural Science Foundation of China, Nos. 31500926 and 81503282, Natural Science Fund of Guangdong Province, No 2014A030310023, Science and Technology Plan of Guangdong Province, Nos. 2014A020212309, 2013B010404044, 2017A01010501
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First we synthesized inhibitor following the
2019-11-15

First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidin
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