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Other karyopherins besides CRM must bind
2020-01-16

Other karyopherins besides CRM1 must bind to FG-Nups in a similar fashion. However, at an atomic resolution, only the interaction of importin β with isolated FG motifs has been analyzed (Bayliss et al., 2000, Bayliss et al., 2002, Liu and Stewart, 2005). Despite similarities in the FG-binding pocket
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br Results br Discussion br
2020-01-16

Results Discussion Conclusions The present study demonstrates that CRF1 receptor-deficiency prolongs whereas CRF2 receptor-deficiency shortens the duration of recognition memory deficits induced by morphine discontinuation, unraveling opposite roles for the two known CRF receptor subtypes i
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br Methods br Results br Discussion Here we have shown
2020-01-15

Methods Results Discussion Here we have shown that two GPCR subtypes thought to trigger similar signalling events by coupling to Gαq in fact regulate different signalling networks via coupling to distinct G proteins. Thus global effects regulated by both receptors in events such as cardiac
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XL228 Are the hydrogens removed simultaneously or one by one
2020-01-15

Are the hydrogens removed simultaneously or one by one? — Δ1-KSTDs can catalyze the exchange of alkali-labile tritium or deuterium atoms at the C2 XL228 of their substrates, even when enzyme turnover was prevented by the absence of an electron acceptor for the oxidative half-reaction [97,98] or by
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Cell migration and invasion are central processes in the
2020-01-15

Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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Acknowledgment This work was supported by the
2020-01-15

Acknowledgment This work was supported by the Swedish Research Council, the Knut and Alice Wallenberg Foundation, the Göran Gustafsson Foundation, the Swedish Pain Relief Foundation, the Torsten Söderbergs Stiftelse, the Swedish Children\'s Cancer Foundation, and the Swedish Cancer Society. The
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Several in vivo human studies have produced conflicting resu
2020-01-15

Several in vivo human studies have produced conflicting results for evaluating the inhibition of OCs on the metabolism of CYP3A substrates. Balogh et al. [12] demonstrated an approximately 25% inhibition of CYP3A activities in vivo after the administration of an OC containing 30μg of ethinylestradio
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From the general synthetic route we first synthesized a dire
2020-01-15

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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br Particle swarm optimization for NLBP br Computational tes
2020-01-15

Particle swarm optimization for NLBP Computational tests Conclusions Acknowledgements This work was supported by the State Key Development Program for Basic Research of China (No. 2009CB421104) and the National Natural Science Foundation of China (Nos. 50809004 & 41071323). Main Text
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br Methods and materials br
2020-01-14

Methods and materials Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic ARM1 to prostaglandin, prostacyclins and thromboxanes., , , Two distinct isoforms of COX were initially discovered: COX-1 is a constitutive, housekeeping enzyme that is expressed in many tiss
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Co operation or synergy between PKA and Epac
2020-01-14

Co-operation or synergy between PKA and Epac has been recently reported in PCCL3 thyroid cell line in which cAMP is pro-mitogenic, in everything to VSMC [19]. Our study demonstrates for the first time that PKA and Epac also synergise to inhibit cell proliferation in a cell type where cAMP in anti-m
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pkc inhibitor br Conclusion The past few years have witnesse
2020-01-14

Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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Introduction Pain is frequently the first
2020-01-14

Introduction Pain is frequently the first clinical symptom of head and neck carcinoma. Indeed, pain is the initial reason leading ∼70% of cancer patients to seek professional assistance (Lam & Schmidt, 2011; Rettig & D’Souza, 2015; Schmidt, 2014). Clinically, cancer-induced facial pain can be evoke
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Our data furthermore suggest that Ch
2020-01-14

Our data furthermore suggest that Ch25h-induced oxysterols could play an important role in modulating the immune cell migration. Mechanistically, we observed impaired trafficking of CD44+CD4+ T cells in mice deficient for Ch25h. CD44+CD4+ T cells lacking EBI2, the receptor of 7α-25OHC, were delayed
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Currently much effort has been
2020-01-14

Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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