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Numerous small molecule CRF receptor antagonists have
2019-09-21

Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121
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br ANTITHROMBOTIC TREATMENTS br VOLUME
2019-09-20

ANTITHROMBOTIC TREATMENTS VOLUME-OUTCOME RELATIONSHIP FOR REVASCULARIZATION PROCEDURES The guidelines also maintain the recommendations for training in PCI, both for ACS (≥ 75 procedures per operator in centers with at least 400 PCI procedures per year and a 24-hour on-call service) and for st
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Kinetic isotope effects KIEs inform
2019-09-20

Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal pyridoxal phosphate of labeled
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It is noteworthy that little is
2019-09-20

It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti
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br Discussion The N terminal domain of DDRs has
2019-09-20

Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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E protein was studied using
2019-09-20

E1 protein was studied using specific anti-E1 (+)-MK 801 in wild type cells and in transfected cells overexpressing the enzyme. The results revealed several unusual characteristics, which are unique to this ubiquitin-activating enzyme. The E1 was translated as a full-length protein and then quickly
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br DDR role in kidney Thirty
2019-09-20

DDR1 role in kidney Thirty-eight papers are reported in PubMed upon the keyword search “DDR1 AND kidney”. Careful examination of those papers shows that only 31 are related to DDR1\'s role in glomerulosclerosis and renal fibrosis, 24 of those being research and the rest review articles. Since the
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Here we found that these leukotriene antagonists also inhibi
2019-09-20

Here we found that these leukotriene antagonists also inhibit the effects of nucleotides acting at P2Y receptors in dU937 cells, which are known to express a number of nucleotide receptors, such as P2Y2 or P2Y4[30]. In an effort to characterize the P2 receptor subtypes subject to negative modulation
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On the basis of the findings described above a
2019-09-20

On the basis of the findings described above, a series of heterotricyclic analogs were designed and synthesized. The human CRF1 receptor binding and antagonist activity data for newly designed heterotricyclic core antagonists 28–33 are described in Table 3. Most of the tricyclic core analogs listed
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Our results show that COX and COX inhibition improve
2019-09-20

Our results show that COX-1 and COX-2 inhibition improve cognitive performance and decrease the neuronal insult during HH. However, when a neuroinflammatory response was observed, COX-1 inhibition was more effective than COX-2 inhibition at reducing microglial activation and augmenting pro-inflammat
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COMT expression protein level and activity are down
2019-09-20

COMT expression, protein level and activity are down regulated by E2. Using estrogen receptor (ER) positive MCF-7 cells, Xie et al. demonstrated an E2 dose dependent (1, 10 and 100 nM) decrease in S-COMT 1.3 kb mRNA that was maximum after 48 h (Xie et al., 1999). A similar decrease was not observed
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86002 br Materials and methods br Results br
2019-09-20

Materials and methods Results Discussion The main finding of the present study is that selective ETA and dual ETA/ETB receptor blockade markedly improve endothelium-dependent vasodilatation in patients with type 2 diabetes and vascular complications. The magnitude of improvement did not dif
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Thus the exact mechanisms responsible for progestogen induce
2019-09-20

Thus, the exact mechanisms responsible for progestogen-induced changes in immune response are not known but the effects are believed to be exerted through receptor-mediated interactions. Since the mPR α is known to be a G protein-coupled receptor in fish, downstream signaling cascades via secondary
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Our results are the first to demonstrate that
2019-09-20

Our results are the first to demonstrate that ERRγ acts as a catabolic regulator of cartilage degeneration and OA pathogenesis, and collectively support the idea that ERRγ could be a therapeutic target for OA Introduction DNA cytosine-5-methyltransferases (Dnmts) catalyze the methyl transfer fr
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Importantly our in vivo data fit to the in vitro
2019-09-20

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 desipramine hcl levels. The doses of XJD used were based on our previous in vivo study (Zhao et al., 201
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