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Given the excellent in vitro pharmacology
2019-07-09
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic AZD2932 functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1 inhib
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Clindamycin HCl weight KSTDs are generally reported to be in
2019-07-09
— Δ1-KSTDs are generally reported to be intracellular enzymes, either soluble or bound to subcellular particles. For instance, the enzymes from C. testosteroni ATCC 11996 and ATCC 17410 [50,90,99], R. equi [29], and N. simplex ATCC 6946 [52] were particulate-bound. On the other hand, the Δ1-KSTDs f
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br CDK Regulators as Coactivators of NF B and
2019-07-09
CDK Regulators as Coactivators of NF-κB and STAT CDK regulating proteins also have the ability to control the inflammatory response. The p21CIP1 protein binds to and inhibits the activity of cyclin–CDK4/6 and cyclin–CDK1/2 complexes. Consistent with its ability to inhibit CDK activity, deletion o
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br Introduction Vitis vinifera L is one of
2019-07-08
Introduction Vitis vinifera L. is one of the most worldwide-grown fruit crop and is mostly used in the wine industry (Bouquet, 2011). Domestication and history changed dramatically the biology of this species and today there are thousands of V. vinifera varieties, being many of them closely relat
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br Acknowledgements br Introduction Serum triglyceride conce
2019-07-08
Acknowledgements Introduction Serum triglyceride concentrations increase following ingestion of a fat containing meal resulting in postprandial hyperlipidemia. Peak serum triglyceride levels are observed within 2 to 4h of fat consumption and then gradually return to baseline levels within appr
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br Results br Discussion Adult hand foot and mouth disease
2019-07-08
Results Discussion Adult hand, foot and mouth disease gets no particular research interest because it has been seen as a sporadic mild viral infection that spontaneously resolved in a few days. However, evidence showed that adults may act as latent enterovirus reservoirs. A serum epidemiologic
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Recent pharmaceutical research in the field of respiratory d
2019-07-08
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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Given that dimethylamine substitution was
2019-07-08
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated nmda receptor amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). Th
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Although it was shown that IL
2019-07-08
Although it was shown that IL-23 signaling induces expression of T17 pathogenic signature genes through activation of STAT3,, transcription factors other than STAT3 are also implicated for induction of pathogenic T17 cells because IL-6, which activates STAT3 similarly to IL-23, cannot induce IL-23R
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Emphysema is an important component of
2019-07-08
Emphysema is an important component of COPD, which is responsible for airflow limitation. In the present study, a significant airspace enlargement was observed 21 days after elastase administration. Interestingly, daily administration of olaparib provided greater protection against emphysema as comp
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In mammals neutrophil elastase is
2019-07-08
In mammals, neutrophil elastase is a trypsin-like serine protease stored in the azurophilic granules of naïve neutrophils [15], [16]. The catalytic activity of neutrophil elastase relies on a His57–Asp102–Ser195 triad (chymotrypsin numbering system) that functions by transfer of electrons from the c
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Our studies approached this problem using integrative
2019-07-08
Our studies approached this problem using integrative -omics analysis of human NK-ieILC1s from distinct microenvironments and functional subsets, including helper and adaptive phenotypes. At both the transcriptional and epigenetic levels, we find that the adaptive subset, CD57+ cytotoxic NK cells, s
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G DH has gained interest because
2019-07-08
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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Numerous studies have pointed to
2019-07-08
Numerous studies have pointed to the DGAT reaction being critical for TAG assembly and in several cases it has been shown to limit carbon flux from lipid precursors towards TAG accumulation [12]. Thus, in Brassica napus, the DGAT substrate, diacylglycerol (DAG), accumulates during periods of rapid l
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br Results br Discussion The
2019-07-08
Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into RF 9 by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by their inhibition
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