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To investigate the mechanism of action of trisubstituted azo
2020-05-08
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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In cholesterol synthesis HMG CoA reductase is the rate
2020-05-08
In cholesterol synthesis, HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins or HMG-CoA reductase inhibitors are commonly used for management of hypercholesterolemia. The presence of an HMG-like moiety on these drugs allows them to competitively bind to the catalytic do
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For the SAR optimization of the right
2020-05-07
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic 1 646 receptor moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by cond
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N-Nonyldeoxynojirimycin synthesis In solid tumors such as th
2020-05-07
In solid tumors, such as those in breast and pancreatic cancer, infiltrating CD68+ or CD163+ tumor-associated macrophages (TAMs) correlate with poor outcome (DeNardo et al., 2011, Kurahara et al., 2011, Shabo et al., 2008). The tumor-promoting function of TAMs is based on their capacity to secrete p
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br Materials and Methods br Acknowledgements br Introduction
2020-05-06
Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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Acknowledgments br PGD is an aracha http www apexbt
2020-05-06
Acknowledgments PGD is an arachadonic acid-derived prostaglandin produced in large quantities when asthmatic lung tissues are challenged by allergens. PGD contracts the airway tissue as well as stimulating an inflammatory response. PGD was also found to be the ligand for a second receptor, DP2 (
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Taken together our results demonstrate that
2020-05-06
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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The current study had the following aims
2020-05-06
The current study had the following 3 aims: Materials and methods Results Discussion Western Europe, USA/Canada, and Australia have traditionally been the areas in which cochlear LY335979 receptor is most common [9], [10]; correspondingly, the most common and well-known validated tests an
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The structures of the set
2020-05-06
The structures of the set of pyrazoles of are contained in the supplied with this manuscript. Acknowledgments Prostaglandin D (PGD) is known to bind with high affinity to two G protein-coupled seven-transmembrane receptors DP1 and DP2. The latter receptor, also known as CRTH2 (chemoattractant
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It has been reported that
2020-05-05
It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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Confidence with which data of animal safety toxicity studies
2020-05-05
Confidence with which data of animal safety/toxicity studies can be translated to human depends upon the knowledge that whether humans would be exposed to similar chemical entities (parent and its metabolites) as the animals exposed during toxicity studies. In this regard, in vitro qualitative evalu
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Materials and Methods br Results br Discussion For
2020-05-05
Materials and Methods Results Discussion For several decades, the diagnosis of translocation-associated childhood sarcomas with overlapping morphological characteristics has been facilitated by pathognomonic gene fusion detection through RT-PCR or FISH. However, these assays have several shor
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br Results br Discussion The advent
2020-05-05
Results Discussion The advent of TKI treatment has greatly improved CML therapy. Because CML LSCs are less sensitive to TKIs, CML is usually controlled rather than cured, highlighting an unmet clinical need. Developed from our previous finding that CML LSCs are more dependent on Tcf1 and Lef1
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br Introduction Lung cancer is the leading cause of cancer
2020-05-05
Introduction Lung cancer is the leading cause of cancer-related death worldwide, accounting for more than 1.5 million deaths in 2012. Non–small-cell lung cancers represent approximately 85% of lung neoplasms; among these, squamous cell carcinomas (SCC) account for approximately 30% of cases. The
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br Material and methods br Results
2020-05-05
Material and methods Results Discussion In the present study, twenty strains of Y. enterocolitica were analyzed for their inhibitory potential on cysteine proteases. Five of these strains belonged to bioserotype 4/O:3, which is distinguished for its pathogenicity towards humans. The rest of
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