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br Conflict of interest statement br References and recommen
2020-11-25
Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We acknowledge financial support by the Swiss State Secretariat for Education, Research and Innovation (Federal
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br Methods br Results br Discussion Here we have
2020-11-25
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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br Conclusions br Declaration of
2020-11-25
Conclusions Declaration of interest Acknowledgements Introduction Uncorrected obesity has been a major health problem and the prevalence of obesity is fast rising reaching an epidemic proportion [[1], [2], [3]]. Ample of clinical and experimental evidence has suggested that obesity leads
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A comparative analysis of the cleavage activity
2020-11-25
A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25
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br Discussion and conclusion Ubiquitination and deubiquitina
2020-11-25
Discussion and conclusion Ubiquitination and deubiquitination have emerged as important mechanisms involved in p53 management. This review revealed that various DUBs can regulate p53 or p53-Mdm2-MdmX networks. Herein, we reviewed the current progress made toward elucidating the complexities in th
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br DUBs in regulation of critical steps in tumor
2020-11-25
DUBs in regulation of critical steps in tumor metastasis Tumor metastasis comprises a complicated series of biological processes in terms of the invasion-metastasis cascade that requires cancer ret inhibitor to (1) migrate and invade from the origin sites through the extracellular matrix (ECM) t
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In the past few years we and others have
2020-11-25
In the past few years we and others have reported that GLP-1 may also be secreted by sub-populations of alpha GSK 2837808A in human pancreatic islets (Marchetti et al., 2012, Ellingsgaard et al., 2011), which could contribute to beta cell function and survival (Marchetti et al., 2012, Ellingsgaard
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The activity of chromenones bearing heteroaryl groups
2020-11-25
The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue
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Another important mediator in fear
2020-11-24
Another important mediator in fear learning is the neuropeptide corticotropin-releasing factor (CRF). For example, local repeated administration of CRF into the basolateral amygdala potentiates the acquisition of cue-conditioned fear (Bijlsma et al., 2011) and CRF1 receptor antagonists effectively b
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they say For the first time we
2020-11-24
For the first time, we provide evidence for COMT Val158Met modulation of long-term fear extinction in humans, evident both in cortical (LPP) and autonomic (fear bradycardia) components of the conditioned fear response. We further found that the initial acquisition of fear is related to dispositiona
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br Materials and methods br
2020-11-24
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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The genetic basis of resistance
2020-11-24
The genetic basis of resistance to dieldrin has been described for several insect species as a mutation in the transmembrane domain II of the GABA-Cl or rdl (resistance to dieldrin) gene (ffrench-Constant et al., 2004; Bass et al., 2004; Du et al., 2005). A mutation in the GABA-Cl gene was found at
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br Particle swarm optimization for
2020-11-24
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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Given the potency enhancing effect
2020-11-24
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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(S)-Methylisothiourea sulfate br Halogenases Enzymatic C H a
2020-11-24
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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