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The present study sought to
2019-12-02
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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MdHCLB channels expressed in Xenopus oocytes produced curren
2019-12-02
MdHCLB channels expressed in Xenopus oocytes produced currents in response to HA and GABA (Fig. 1, Fig. 3). This is in agreement with the findings with Drosophila HCLB channels (Gisselmann et al., 2004). In the HA concentration-response curves, the effects of GABA were additive to those of HA only i
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br Materials and methods br Results We examined the effects
2019-12-02
Materials and methods Results We examined the effects of curcumin in Fluo-4 loaded SH-EP1 (±)-Bay K 8644 stably transfected with human α7-nACh receptor. Application of curcumin alone in the concentrations up to 100 μM for 30 sec. did not induce any detectable change in intracellular Ca2+ leve
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From a mechanistic standpoint the BCL RD domain represses
2019-12-02
From a mechanistic standpoint, the BCL6 RD2 domain represses the GPR183 and S1PR1 loci by recruiting HDAC2, but not MTA3-NuRD, to suppress the enhancer activation mark H3K27ac at their distal regulatory elements. However, these data do not exclude the possibility that other as yet unknown corepresso
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Because EBI is expressed on the major subsets of immune
2019-12-02
Because EBI2 is expressed on the major subsets of immune cells, and small molecule antagonists for EBI2 were recently described (Benned-Jensen et al., 2013, Gessier et al., 2014), EBI2 constitutes a tempting drug target reminiscent of the sphingosine-1-phosphate receptor superagonist fingolimod/Gile
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br Concluding Remarks Recent studies have
2019-12-02
Concluding Remarks Recent studies have provided unprecedented details of APC/C structure and enzymology, which explain how the activity of this massive E3 ligase is controlled, and how ubiquitylation is achieved to temporally regulate cell division. Although one pervasive question has been why th
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Muscle Ring Fingers MuRFs comprising TRIM MuRF TRIM
2019-12-02
Muscle Ring Fingers (MuRFs) comprising TRIM63 (MuRF1), TRIM55 (MuRF2) and TRIM54 (MuRF3) are the most studied TRIMs in the heart. However, with increasing knowledge of E3 ligases and recent advancements in the field, many other TRIMs such as TRIM8, TRIM21, TRIM24, TRIM32, TRIM45, TRIM69 and TRIM72 w
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In addition to through direct regulation of cell
2019-11-30
In addition to through direct regulation of cell differentiation, DDR2 may raise the abundance of myofibroblast subsets through advancing the recruitment of its precursor cells. One such evidence is that DDR2 can regulate lung fibroblast proliferation and migration. Another possibility rests on the
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The on target in vitro pharmacology of was then further
2019-11-30
The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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Flavonoids are most common and widely distributed group
2019-11-30
Flavonoids are most common and widely distributed group of natural phenolic compounds synthesized by plants that have varied effects on mammalian cell systems (Kumar and Pandey, 2013). Several studies demonstrate that flavonoids might be potent inhibitors of several protein kinases involved in vario
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br Experimental procedures br Acknowledgments
2019-11-30
Experimental procedures Acknowledgments Introduction Receptor tyrosine kinases (RTKs) control many fundamental cellular processes, such as cell proliferation, differentiation, migration, and metabolism (Lemmon and Schlessinger, 2010). RTK activity is normally tightly controlled, and dysregu
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Increased levels of PCNA monoubiquitination by UbL P express
2019-11-30
Increased levels of PCNA monoubiquitination by UbL73P expression in a damage-independent manner mimics the phenotype observed for USP1 knockdown (Huang et al., 2006, Jones et al., 2012). USP1 is the only DUB to date shown to remove ubiquitin from PCNA in vivo. This finding reveals the highly dynamic
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DNA PK Jackson is activated by DNA
2019-11-30
DNA-PK (Jackson, 1997) is activated by DNA double-stranded breaks (DSBs). It is a trimeric complex composed of the catalytic subunit, DNA-PKcs, and the Ku70/80 heterodimer. DNA-PK mediates non-homologous end joining (NHEJ), which joins programmed DSBs created during V(D)J recombination and class swi
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pave a road br Acknowledgments br Casein kinases CK are seri
2019-11-29
Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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For the current studies we used the selective Epac agonist
2019-11-29
For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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