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51 3 kinase To develop novel EPAC inhibitors
2019-09-25
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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QSAR based on the D structures of ligands
2019-09-25
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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br Conflict of interest br
2019-09-25
Conflict of interest Acknowledgments Part of this work was supported by Institut Francais en Egypte, and the Academy of Scientific Research and Technology in Egypt under the frame of “Imhotep Project N°: 31681XL” and “STDF/IFE project N° 30630″ Introduction NSAIDs play an important role in
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Other membrane currents are affected
2019-09-25
Other membrane currents are affected as well. Some studies have provided evidence that sulfonylureas, in addition to blocking KATP channels, also inhibit chloride and calcium channels. GLYB has been shown to almost inhibit the current generated by Na+–K+ pumps in a concentration-dependent manner (wi
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iso 1 kinase Introduction Primitive neuroectodermal tumors P
2019-09-25
Introduction Primitive neuroectodermal tumors (PNETs) are malignant, small round cell tumors of neural crest origin which typically arises from bone or soft tissue in the trunk/axial skeleton/paraspinal regions in adolescents and young adults and comprises of 50% cases with local recurrence and met
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In conclusion we provide convincing
2019-09-25
In conclusion, we provide convincing evidence that the PRRSV-induced SGs are indeed bona fide SGs. While we determined that mRNA is present in the PRRSV-induced SGs, we did not distinguish its origin. Future studies will need to determine whether the mRNA stored in PRRSV-induced SGs is of cellular o
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In the present study real time polymerase chain
2019-09-25
In the present study, real-time polymerase chain reaction also confirmed that gene expressions of RT1 class II, locus Bb (RT1-Bb) was up-regulated and Spi-B transcription factor (Spib) was downregulated at day 3 after the VMH lesions. These two genes work as one of immune responses. RT1-Bb controls
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Domiphen Bromide clinical An analysis of EBI expression on
2019-09-25
An analysis of EBI2 expression on dendritic cells (DCs) showed that EBI2 is highly expressed on CD4+ conventional cDCs. In line with this mice deficient for EBI2 largely lack this subset of cDCs in the spleen. Furthermore, the localization of the residual cells is disturbed [10,11]. It was found tha
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Gastrointestinal tone can be effectively modulated
2019-09-24
Gastrointestinal tone can be effectively modulated by cholinesterase inhibitors. As parasympathetic fibers release no sodium salt to contract the circular and longitudinal intestinal muscles, AChE inhibition can facilitate those actions. Postoperative ileus (delayed gastric emptying after surgery)
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AON successfully alleviated the myotonic phenotype in DM
2019-09-24
AON successfully alleviated the myotonic phenotype in DM model mice [18], [23]. To screen for an optimal AON sequence, we used 25-mer phosphorothioate 2′ O-methyl RNA molecules that covered the exon 6B or exon 7A. Unexpectedly, AON 7A (+63−8) which covers the boundary of intron 7A and exon 7A enhanc
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br Acknowledgements br Introduction L Rhamnosidases EC are
2019-09-24
Acknowledgements Introduction α-L-Rhamnosidases (EC 3.2.1.40) are glycosyl hydrolases (GHs) that cleave terminal α-l-rhamnose from a large number of natural products [1]. The action of α-L-rhamnosidases (α-RHAs) has been reported, among others, on different complex substrates such as heteropol
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Epirubicin HCl br DDR receptor and MMP
2019-09-24
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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br Author Contributions br Acknowledgments br
2019-09-24
Author Contributions Acknowledgments Introduction Osteoporosis is a common bone disease that frequently leads to disruption of the alveolar and systemic bones with age. Novel osteoanabolic strategies to treat osteoporotic bone loss or augment fracture repair efficiently are desired. Since b
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Alpha SYN has no direct effect on forskolin induced
2019-09-24
Alpha-SYN has no direct effect on forskolin-induced CREB phosphorylation, but rather blocks the stimulation of CRE-mediated transcription in the nucleus. Previously we suggested that α-SYN can enter the nucleus and is present in both cytosolic and nuclear fractions without direct interaction between
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PEG Virus Precipitation Kit A second advance came with
2019-09-24
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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