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Given its high frequency it is not surprising that different
2019-12-02
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant (+)-Bicuculline sale to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have
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br Lymphoplasmacytic lymphoma Waldenstrom macroglobulinemia
2019-12-02
Lymphoplasmacytic lymphoma/Waldenstrom macroglobulinemia Lymphoplasmacytic lymphoma (LPL) and its subgroup Waldenstrom macroglobulinemia (WM) are rare and indolent lymphomas that arise from fully differentiated B cells. The only family of GPCRs that has been well studied in LPL/WM is the chemokin
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Isochlorogenic acid C Moving forward the new mathematical mo
2019-12-02
Moving forward, the new mathematical model opens doors for understanding the SCF network, where activity of a component is blunted through mutation or altered in expression in diseased states, and during therapeutic intervention. Computational modeling could reveal underappreciated secondary or tert
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How does an increase in E affinity
2019-12-02
How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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Resveratrol is a phytoalexin that occurs
2019-11-30
Resveratrol is a phytoalexin that occurs in relatively large amounts in peanut, berries, grapes, and red wine (Soleas et al., 2001). A recent study showed that resveratrol prevents social deficit in an animal model of autism, indicating its potential for possible therapeutic use in children with aut
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A neurotoxic syndrome called Intermediate
2019-11-30
A neurotoxic syndrome called “Intermediate syndrome” has been described after acute cholinergic crisis, which has been interpreted as the result of pre- and postsynaptic disruptions of neuromuscular transmission (Senanayake and Karalliedde, 1987). Other toxic effects with unknown molecular targets h
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As the primary model we selected
2019-11-30
As the primary model we selected LDL-receptor knockout mice because these resemble the human plasma lipoprotein profile more closely. Currently, genetic models with reduced milk cholesterol content, which mimic cholesterol-free formula feeding, are unavailable. Thus, instead of modifying milk choles
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br Introduction Oral contraceptives OCs are the
2019-11-30
Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol
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Given the potency enhancing effect of the butyl group
2019-11-30
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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Structural changes within the heteromer induced by agonist
2019-11-30
Structural changes within the heteromer induced by agonist administration show a high level of complication. The presented results obtained in quantitative FLIM-FRET measurements with two selective ligands match the qualitative conclusions indicated by changes in the intracellular calcium level. The
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cGAS has a central role in STING activation after DNA
2019-11-30
cGAS has a central role in STING activation after DNA sensing, but it is unknown if most of the DNA sensors act independently or in cooperation with the cGAS-cGAMP pathway. This was addressed for IFI16 (Almine et al., 2017, Jønsson et al., 2017) and PQBP1 (Yoh et al., 2015) but remains to be tested
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DGK is classified into the
2019-11-30
DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a
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In conclusion this study provides the first
2019-11-29
In conclusion, this study provides the first investigation of role of ACC receptors in parasitic nematodes. While research using C. elegans to evaluate anthelmintic targets is an excellent tool to provide relevant information, research on similar targets in parasitic nematode can provide key informa
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It seems plausible that this ESC driven effect relies
2019-11-29
It seems plausible that this ESC-driven effect relies on a paracrine signaling. Numerous studies showed that the Fgf4 (fibroblast growth factor 4)/MAPK (mitogen-activated protein kinase) pathway is involved in PE differentiation in mouse L-Cysteinesulfinic acid (Chazaud et al., 2006), (Frankenberg
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Another milestone in the field is the de novo discovery
2019-11-29
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of 8-Bromo-cGMP, sodium salt synthesis , it has been widely applied as a useful chemical probe to discriminate EPAC related
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