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Compounds and administered orally to fasted Harlan
2019-12-24
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinical
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br Transparency document br Acknowledgments This
2019-12-24
Transparency document Acknowledgments This work was supported by the Ministry of Education, Youth and Sports of the Czech Republic (the National Program of Sustainability I, Grants LO1204 and LO1304), by the Czech Science Foundation (15-17282Y) and by Palacký University Olomouc (IGA_PrF_2017_0
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We observed the IVM potentiation
2019-12-24
We observed the IVM potentiation of currents induced by the EC5 of Glu or GABA and the IVM inhibition of currents induced by the EC90 of Glu or GABA in wild-type GluCls and GABACls. The EC50 of IVM for the potentiation in GluCls was 3.5-fold smaller than that in GABACls (Fig. 4, Fig. 8B, Table 2), a
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Introduction Penetrator with Enhanced Lateral
2019-12-24
Introduction Penetrator with Enhanced Lateral Effect (PELE) is a kind of ammunition which consists of a low-density material as the filling and a high-density material as the jacket [1,2]. When PELE impact target, the jacket is radially accelerated, expanded and fractured because of distinctive lat
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Baicalein trihydroxyflavone was first isolated from the root
2019-12-24
Baicalein (5,6,7- trihydroxyflavone) was first isolated from the roots of Scutellaria baicalensis Georgi (Lamiaceae family), a medicinal plant with diverse therapeutic implications; antibacterial, antiviral, and anti-inflammatory properties. It has been found that baicalein benefits neuroinflammatio
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kv1.3 inhibitor To identify and characterize new
2019-12-24
To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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br Cytochrome P monooxygenases Cytochrome
2019-12-24
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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br Introduction Cerebral stroke causes an efflux of
2019-12-24
Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t
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Our research has demonstrated that the absolute bioavailabil
2019-12-24
Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin
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In the phase I AURA trial patients with
2019-12-24
In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for NECA 19 deletions, 86% for L858R and 70
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Oxysterols modulate the immune responses and as such could
2019-12-24
Oxysterols modulate the immune responses and as such could be effectors of the tumor environment: 25-OHC impairs IgA production in B-lymphocytes [26] and induces the secretion of the proinflammatory and angiogenic cytokine IL-8 [27], [28]. Of note, oxysterols (in particular 7α,25-OHC) are potent che
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br Author contribution br Acknowledgements We want to thank
2019-12-24
Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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br RING type E s and their
2019-12-23
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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Collagen compaction and alignment are generated by cell medi
2019-12-23
Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano
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The structure of the HOIP RBR LDD module bound to
2019-12-20
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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