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Introduction The Discoidin Domain Receptors DDRs comprising
2020-06-28
Introduction The Discoidin Domain Receptors (DDRs), comprising DDR1 and DDR2, are collagen-binding receptor tyrosine kinases (RTKs) that function as microenvironmental sensors at the interface of the extracellular matrix and the intracellular signal transduction machinery [1]. In response to ligand
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We have previously reported DAPK inhibitors discovered throu
2020-06-28
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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The changes in the chemokine receptors CCR and CXCR
2020-06-28
The changes in the chemokine receptors CCR-5 and CXCR-4 in women and men with PTSD are completely different. In the group of women with PTSD alone the level of this Cilnidipine increased six times, whereas, in women with APD and PTSD, the level of the receptor CCR-5 was eight times higher than in t
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Chk and Chk are functionally redundant protein kinases that
2020-06-28
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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Several CHK inhibitors have been
2020-06-28
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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What is the predominant mechanism underlying the benefits of
2020-06-28
What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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br Introduction Cell transplantation therapies using
2020-06-28
Introduction Cell transplantation therapies using embryonic stem cell (ESC) and induced pluripotent stem cell (iPSC)-derived retinal tissue (ESC/iPSC retina) or nf-κb pathway have emerged as therapeutic options for retinal degeneration following recent breakthroughs. A number of groups have shown
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NCT-502 In addition to PGC transcriptional co repressors
2020-06-28
In addition to PGC1α, transcriptional co-repressors such as NCOR and RIP140 participate in oxidative muscle remodeling induced by exercise, whereby reductions in their expression and the resulting de-repression of downstream TFs activates oxidative gene expression (Seth et al., 2007, Yamamoto et al.
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br Activatable photoacoustic probes Photoacoustic PA imaging
2020-06-28
Activatable photoacoustic probes Photoacoustic (PA) imaging is a recently developed technique [47]. The imaging approach uses probes that absorb a pulsed laser beam and convert light energy into acoustic signals. It combines the advantages of the high sensitivity offered by optical imaging and th
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2×Taq PCR Master Mix(with dye) Glycolysis is important
2020-06-28
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its 2×Taq PCR Master Mix(with dye) metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites
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br Conflict of interest br Acknowledgements
2020-06-28
Conflict of interest Acknowledgements This work was supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP: 2014/00926-3). Introduction The metacestodes of Taenia solium are the causative agent of cysticercosis, which mainly resides the skeletal muscles and the central n
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br Signaling of DDR receptor and its
2020-06-28
Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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To analyze EBI expression and its function in T cells
2020-06-28
To analyze EBI2 expression and its function in T cells in vivo, we created an EGFP reporter/knockout mouse strain, termed EBI2EGFP. This mouse strain in heterozygous configuration allows for a systematic analysis of the expression of EBI2 in distinct cell types in steady-state and under inflammatory
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br Results br Discussion Taking advantage of the
2020-06-28
Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate PD 169316 sale that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2 interacti
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br Additional CDKs with a role
2020-06-24
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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