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Because stimulation and blockade of dopamine D receptor
2019-12-30

Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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The aniline R group was extensively explored and a
2019-12-30

The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series
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Chk and Chk are functionally redundant protein kinases
2019-12-29

Chk1 and Chk2 are functionally redundant protein kinases that respond to checkpoint signals emanating from the phosphatidylinositol 3-kinase family members ATM (ataxia-telangiectasia mutated) and ATR (Ataxia-telangiectasia and Rad-3 related). A concerted research effort has revealed many mechanistic
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br Acknowledgements br Introduction Ischemic retinopathy is
2019-12-29

Acknowledgements Introduction Ischemic retinopathy is common to the major causes of blindness, including proliferative diabetic retinopathy, venous occlusion, and retinopathy of prematurity. The hypoxia that follows retinal capillary obliteration drives deregulated growth of new blood vessels
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In different body organs a
2019-12-29

In different body organs, a number of biological functions are generally mediated by binding of the extracellular substances to the particular transmembrane receptors, which results in subsequent signal stimulation by intracellular signaling cascades. These cascades function over the complex network
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The focus of this review is on the
2019-12-29

The focus of this review is on the diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) enzymes, DGAT1 and DGAT2, that catalyze the esterification of a fatty acyl moiety to a DAG molecule to produce TAG. These enzymes commit DAG to being stored as TAG rather than being diverted for the synthesis of ph
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It is well established that Shp can function as
2019-12-29

It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed
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Defensins are one major class of antimicrobial cationic
2019-12-29

Defensins are one major class of antimicrobial, cationic peptides that are released from Epidermal Growth Factor (EGF), human recombinant receptor and imbedded in the mucus layer on mucosal surfaces [45]. They can be categorized into two major families; α- and β-defensins. In humans there are two α-
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As the principal receptors for regulating the inflammatory p
2019-12-29

As the principal receptors for regulating the inflammatory process in mammals, CXCR1 and CXCR2 have an important role in regulating the trafficking of phagocytes such as neutrophils, monocytes and macrophages (Viola and Luster, 2008). The evidence gathered to date from fish studies are in agreement
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We have previously disclosed the discovery of
2019-12-29

We have previously disclosed the discovery of a 7-azaindole-3-acetic oxygenase CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work, o
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br Introduction Al Awqati and his
2019-12-29

Introduction Al Awqati and his colleagues using R(+)-methylindazone, R(+)-[(6,7-dichloro-2-cyclopentyl-2,3-dihydro-2-methyl-1-oxo-1H-inden-5-yl)-oxy] acetic p-nitro-Cyclic Pifithrin-α (IAA-94) (Landry et al., 1987) isolated the first chloride intracellular ion channel (CLIC) proteins (p64) from b
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Deregulated Wnt signaling either due to pathway
2019-12-29

Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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Under conditions of energy scarcity or
2019-12-29

Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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br Results and discussion br
2019-12-29

Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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Oxidative stress is associated with
2019-12-29

Oxidative stress is associated with elevated levels of intracellular reactive oxygen species (ROS) generation which then causes DNA damage and the death of cells (Miyata et al., 2017). Generation of ROS affects main signaling pathways in cells associated with tumorigenesis: mitogen activated protein
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