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In the course of an
2021-11-11
In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pr
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Neuropathic pain NP is a chronic pain caused by
2021-11-11
Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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TRRAP participates in embryonic development as
2021-11-11
TRRAP participates in embryonic development, as demonstrated by its binding with proteins regulating the Notch signaling pathway in fruit fly, the Ras signaling pathway in C. elegans, or the Wnt signaling pathway in 293T cells. Therefore we suspect that TRRAP variants, more especially those falling
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Experimental conditions may be critical to explain one model
2021-11-11
Experimental conditions may be critical to explain one model or the other. The matter of Hippo-driven cytoplasmic sequestration (Varelas et al., 2008) of active SMAD complexes (Varelas et al., 2008) vs. TßR basolateral relocalization upon epithelial polarization (Nallet-Staub et al., 2015) as mechan
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br Introduction Sister chromatid cohesion
2021-11-10
Introduction Sister-chromatid cohesion is established during DNA replication by a ring-shaped cohesin complex consisting of the core subunits Smc1, Smc3, Scc1, and SA1 or SA2, which recruit regulatory subunits Pds5 (Pds5A/B in vertebrates), Wapl, and Sororin to regulate the association of cohesin
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Although some PAHs that are human carcinogens have
2021-11-10
Although some PAHs that are human carcinogens have been found in the sugarcane soot (Zamperlini et al., 1997), there are no data about cancer incidence among sugarcane workers. To the best of our knowledge, this is the first report of an evaluation of internal exposure, comparing the harvesting (whe
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Although glycine receptors predominate in the brain
2021-11-10
Although glycine receptors predominate in the brain stem and spinal cord, they are also expressed in higher brain regions such as the nucleus accumbens, frontal cortex, and hippocampus (Jonsson et al., 2012, Jonsson et al., 2009, Molander and Söderpalm, 2005b). A variety of drugs of abuse, including
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The overall very satisfactory potency profile
2021-11-10
The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic ci-1033 core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sensi
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The highest metabolic stability observed for compound k EC
2021-11-10
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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AGK 2 br Acknowledgements This work was in part
2021-11-10
Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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br RESULTS br DISCUSSION In
2021-11-10
RESULTS DISCUSSION In this study, we found impaired apoptosis in the peripheral blood of RA patients when compared with peripheral blood from normal controls. Our previous studies have shown that the number of CD4 + T NPE-caged-proton mg increased while regulatory T (Treg) cells diminished in
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Contrary to the transient nature of signal transmission
2021-11-10
Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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Patients with SCI often develop chronic neuropathic pain
2021-11-10
Patients with SCI often develop chronic neuropathic pain, which further deteriorates their quality of life [5]. This condition results from functional and structural plastic changes that occur centrally following injury to spinal cord neurons and glia, and include changes in receptor function and si
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Integrase inhibitors have been licensed for
2021-11-10
Integrase inhibitors have been licensed for use in the UK since 2008. BHIVA now recommend starting all treatment naïve patients on a regimen containing two NRTIs, plus one of the following: a ritonavir boosted PI, an NNRTI, or an integrase inhibitor. They make further recommendations for patients wi
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br Introduction Erythropoietin EPO is a glycoprotein hormone
2021-11-10
Introduction Erythropoietin (EPO) is a glycoprotein hormone and the principal stimulator of erythropoiesis (Jelkmann, 2011). EPO promotes the proliferation and differentiation of red blood cells, which is important for oxygen transport. Low EPO levels in blood cause anemia; however, excessive lev
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