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To develop novel EPAC inhibitors Zhou
2020-04-13
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dockin
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br Acknowledgement We acknowledge for funding support
2020-04-13
Acknowledgement We acknowledge for funding support from Maryada Foundation, a DoD/Army Contract No. W911NF-06-1-0095, and National Institutes of Health through the New England Center of Excellence for Biodefense (Grant AI057159-01). Introduction The Gram-negative bacterium Lysobacter sp. XL1
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Introduction Activation of epidermal growth
2020-04-13
Introduction Activation of epidermal growth factor receptor (EGFR)-receptor tyrosine kinases (RTKs) is a key factor in the progression of non-small cell lung cancer (NSCLC). EGFR-RTKs cause proliferation, invasion, metastasis, and angiogenesis, as well as suppress apoptosis, in lung adenocarcinoma
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Liquidambaric acid br Conclusions When the authors joined th
2020-04-13
Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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Another breakthrough towards the understanding of
2020-04-13
Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t
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The synthesis of tricyclic analogs is
2020-04-13
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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The present study failed to
2020-04-13
The present study failed to demonstrate an independent association of preoperative ChE with BCR. This is in contrast to Koie et al. who reported that pretreatment serum ChE was significantly associated with BCR in 535 patients with CaP who underwent RP (5-year BRFS rates were 77.7% and 55.0%, respec
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Ten non FH ADH probands
2020-04-13
Ten non-FH ADH probands fulfilled the diagnostic criteria of hyperabsorbers. Table 2 shows the main lipid characteristics of these subjects and of 10 non-hyperabsorber probands used for comparison. There were differences between groups in body mass index, waist circumference and triglycerides. Other
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Our study shows that deletion of Dpf in
2020-04-13
Our study shows that Mouse iPSC Chemical Reprogramming Cocktails Kit plus synthesis of Dpf2 in mouse ESCs decreased their self-renewal ability and dramatically impaired their differentiation into mesoderm and endoderm while promoting neural ectoderm differentiation. The differentiation defect to me
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The action of pt PGE as an EP receptor agonist
2020-04-13
The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in
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In order to gain further
2020-04-10
In order to gain further insights into the role of peptidases in B. xylophilus, four cysteine proteases highly secreted by B. xylophilus (Cardoso et al., 2016) were selected four further characterisation. Materials and methods Results and discussion Structural prediction and analysis The i
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Our results in the present
2020-04-10
Our results in the present study demonstrate that CysLT1 mediates leukotriene-induced contraction in the fundus and suggest that both CysLT1 and CysLT2 mediate leukotriene-induced contraction in the antrum in vitro. Further studies on the effects of leukotrienes in vivo are required to elucidate the
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br Experimental Procedures br Acknowledgments
2020-04-10
Experimental Procedures Acknowledgments Introduction The ability of the affiliative and nurture hormone oxytocin (OT) to attenuate stress has been observed across psychological, neurological, and physiological levels [1], [2]. We and others have demonstrated that, in the gut, OT can lessen
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Finally we demonstrated for the first time that the physiolo
2020-04-10
Finally, we demonstrated for the first time that the physiological combinations of estradiol and progesterone levels of premenopausal and postmenopausal women efficiently stimulated the growth of T47D spheroids while clinically relevant concentrations of TPA and UPA suppressed the growth of T47D sph
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In mammals ribonucleotide reductase RNR is a unique enzyme
2020-04-10
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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