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br Substoichiometric substrate modification E ligases
2019-08-15
Substoichiometric substrate modification E3 ligases catalyze the rapid transfer of the SUMOD from the E2 enzyme to the substrate. By definition, enzymes are recycled in the reaction, allowing multiple rounds of substrate modification by a single enzyme. Thus, enzymes function at substoichiometric
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Thiorphan Elevated DPP activity has been strongly associated
2019-08-15
Elevated DPP-4 activity has been strongly associated with diabetes mellitus, IR (Röhrborn et al., 2015), metabolic syndrome (Lamers et al., 2011) and inflammation (Zhong et al., 2015). However, report has it that GC exposure increases DPP-4activity in thymocyte homogenates (Kraml et al., 2003) but t
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Herein in continuation of our interest in
2019-08-15
Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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Thus RhoA mediated inhibition of
2019-08-15
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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Elevated production of cysLTs in asthma and rhinitis in
2019-08-15
Elevated production of cysLTs in Phosphatase Inhibitor Cocktail (2 Tubes, 100X) and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of
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The consistent anti anxiety effects obtained with intra mPFC
2019-08-15
The consistent anti-anxiety effects obtained with intra-mPFC injections of CP 376395 strongly suggest a tonic role of CRF at CRF1 receptors located within this limbic GPCR Compound Library area in the modulation of anxiety in the mouse on the EPM. Intra-mPFC injection of CP 376395 led mice to explo
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Interestingly Carver Johnson and Kim investigated a polymorp
2019-08-15
Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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No effect on the A production by
2019-08-15
No effect on the Aβ production by γ-secretase was observed at 50μM, the highest effective concentration used in cultured Neuromedin B by the study of Flajolet et al. IC261 did also not exert a modulatory effect on the production of Aβ, Aβ and Aβ species in the cell-free assay at this concentration.
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Cycloheximide br Experimental procedures br Introduction Pro
2019-08-15
Experimental procedures Introduction Protein kinases represent one of the largest enzyme Cycloheximide in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activity, targ
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A surprising second functional effect was found
2019-08-15
A surprising second functional effect was found in culture experiments. Inclusion of LTD4 reduced the frequency of Fas receptor (CD95) expression. Once again, this effect, although modest, was reversed by a cysLT1 receptor antagonist. The biologic significance of this effect or its mechanism remaine
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Cells expressing the CDK S D
2019-08-15
Cells expressing the CDK5 S47D mutant exhibit impaired migration and enhanced proliferation: Finally, we wished to determine the functional significance of this phosphoevent. Multiple studies have implicated active CDK5 in promotion of cell migration [9,16,[21], [22], [23], [24]] and in one study th
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While a number of studies have helped elucidate the
2019-08-14
While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub checkpoint activity specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in govern
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While SCF E ligase activity was reconstituted
2019-08-14
While SCF E3 ligase activity was reconstituted with recombinant proteins two decades ago, the ability to probe APC/C was limited until recently because of its behemoth size. Human APC/C is a 1.2-MDa assembly comprised of 19 core subunits (one each of nine different APC subunits, and two each of five
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The Inhibitor of APoptosis IAP proteins were first
2019-08-14
The Inhibitor of APoptosis (IAP) proteins were first identified as gene products of baculovirus that inhibited apoptosis of infected insect Etoposide (Clem et al., 1991, Crook et al., 1993). Subsequently, the mammalian IAP family was identified (Rothe et al., 1995, Uren et al., 1996). All members o
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Until recently the first line treatment of RLS was the
2019-08-14
Until recently, the first line treatment of RLS was the administration of low dose of three dopaminergic drugs, which has been approved by the US Food and Drug Administration and the European Medicines Agency for the treatment of moderate to severe RLS. These compounds are pramipexole (Mirapex), rop
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