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br Methods and materials br Results br Discussion In
2021-09-29
Methods and materials Results Discussion In this study we demonstrate that CF epithelial indacaterol receptor exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors responsi
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Our observation of LPS induced increase in the sensitivity o
2021-09-29
Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary Rofecoxib towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, the possible re
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topotecan sale br Conclusions In this study we report the ge
2021-09-29
Conclusions In this study, we report the genotype frequencies for GSTT1, GSTP1, and GSTM1 in Jamaican children. The frequency of the null genotypes of GSTT1 and GSTM1 are similar to those of African-Americans in the US. The GSTP1 genotype frequency is closer to that of the African-American popula
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The number of small molecule
2021-09-29
The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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br Conclusion In this report we describe the
2021-09-29
Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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calcium channel blocker Introduction Glycogen synthase kinas
2021-09-29
Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and calcium channel blocker is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsoli
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ACET receptor br Next we explored the SAR around the aryl
2021-09-29
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic ACET receptor sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did no
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For another the N terminal sequence of native
2021-09-29
For another, the N-terminal sequence of native glucagon is highly conserved, and positions 8, 9, 16 and 18 are noteworthy in maintaining glucagon activity [18], [20], [21]. It also achieves a degree of selectivity from its C-terminal residues, and a significant contribution is made by the C-terminal
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br Author contributions br Transparency document br Acknowle
2021-09-28
Author contributions Transparency document Acknowledgments The financial contributions of the Marie-Curie Action: BIOCONTROL, contract number MCRTN – 33439, the Agence Nationale de la Recherche (projects membraneDNP 12-BSV5-0012, MemPepSyn 14-CE34-0001-01, InMembrane 15-CE11-0017-01 and the
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br The HDC knockout mouse as a pathophysiological model of
2021-09-28
The HDC knockout mouse as a pathophysiological model of TS The implication of a hypomorphic allele of the Hdc gene as a rare cause of TS (Ercan-Sencicek et al., 2010) created a rare opportunity for the generation of a pathophysiologically grounded model of the disorder. Modeling pathophysiology o
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br Resistance to targeted therapy The idea
2021-09-28
Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target
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Heme activates the master regulator
2021-09-28
Heme activates the master regulator of the anti-oxidant stress response, NRF2, which mediates the up-regulation of a battery of phase II detoxifying genes [106]. Remarkably, HO-1 induction by NRF2 is regulated via an interplay with the transcriptional repressor BACH1 at the Maf recognition zingerone
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br Trifluoromethylketones This group of compounds was demons
2021-09-28
Trifluoromethylketones This group of compounds was demonstrated to bind the zinc thyrotropin releasing hormone in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene a
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Toxoplasma gondii is an exceptionally
2021-09-28
Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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telomerase inhibitor Introduction Multiple sclerosis MS a ne
2021-09-28
Introduction Multiple sclerosis (MS), a neurological autoimmune disease, is driven by CD4+ telomerase inhibitor of the T helper (TH) cells [1]. There is no curative treatment for MS and the present treatments typically focus on immunomodulation for slowing the progression of the disease. These inc
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