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The efficacy of A in the ob ob
2020-10-29

The efficacy of A-922500 in the ob/ob mouse model is of particular interest for two reasons. One of the most striking features of the DGAT-1 deficient mouse phenotype is the resistance to diet-induced obesity (Smith et al., 2000). However, SBI-0206965 of DGAT-1 in leptin deficient ob/ob mice failed
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Preliminary studies evidenced the presence
2020-10-29

Preliminary studies evidenced the presence of CRFr in gamma-aminobutyric acid-ergic (GABAergic) neurons of the hippocampus (Yan et al., 1998). In fact, in this Chidamide area, CRF inhibits glutamate release through CRF1r (Bagosi et al., 2015), leading to a decrease in the GABA concentration in the
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br Financial Support We would like to acknowledge financial
2020-10-29

Financial Support We would like to acknowledge financial support by the National Natural Science Foundation of China (grant numbers 81672778 and 81372165) and Natural Science Foundation of Beijing Municipality (grant number 5142009). Acknowledgements Introduction The process of spermatogen
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From our array results Supplemental Fig S we found
2020-10-29

From our array results (Supplemental Fig. S2), we found that differential lncRNA profiling exhibited much greater disparity compared to differential gene profiling in CD28nullCD8+ T cells, indicating that differentially expressed lncRNA(s) would serve as ideal hallmarks. Moreover, we were fortunate
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br Acknowledgements We are grateful to the National Natural
2020-10-29

Acknowledgements We are grateful to the National Natural Science Foundation of China (Grant Nos. 21571033 and 81503099) and the New Drug Creation Project of the National Science and Technology Major Foundation of China (Grant No. 2015ZX09101032) for financial aids to this work. The research was a
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We have previously reported the characterization of A a nove
2020-10-29

We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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Udenafil also has shown the ability to significantly inhibit
2020-10-29

Udenafil also has shown the ability to significantly inhibit the decrease of vascular endothelial cell function and inhibit the decrease in endothelial cell and smooth muscle contents, thus preventing their fibrosis within the penile corpus cavernosum in diabetic or hyperlipidemic animal models when
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In the literature we can
2020-10-29

In the literature, we can find two different modes of action for estrogens: Firstly there is the commonly accepted genomic pathway. Estrogens pass the cell membrane due to their lipophilic character via diffusion and bind to estrogen receptors (ERs) in the cytoplasm. After binding a dimerization of
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When women reach the menopause they experience
2020-10-29

When women reach the menopause they experience a number of physical complaints such as hot flushes, vaginal dryness and mood changes [1]. Bone loss also becomes manifest at this time [1], [2], but women will often not suffer from back pain before a vertebral fracture occurs. Women who have had one f
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The potent estrogen EE induced a
2020-10-29

The potent Aurora Kinase Inhibitor III EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) w
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In general cellular senescence is
2020-10-29

In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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Thus RhoA mediated inhibition of DGK is
2020-10-29

Thus RhoA-mediated inhibition of DGKθ is a well-characterized pathway, conserved from C. elegans to mammalian tissues, which enables G-protein coupled receptors to regulate the extent and kinetics of DAG-mediated signaling by fine tuning DGK enzymatic activity. Acknowledgments Introduction Ce
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Acknowledgments We are grateful to
2020-10-29

Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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One possible explanation for differences in the binding abil
2020-10-29

One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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pka inhibitor Palliative surgeries for refractory epilepsy i
2020-10-28

Palliative surgeries for refractory epilepsy include vagus nerve stimulation and corpus callosotomy. Among 220 individuals with CDD with parent-entered data, 17% had a vagus nerve stimulation implanted and 69% of parents reported reduced seizure frequency. These data are consistent with a case repor
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