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Several CHK inhibitors have been
2021-01-25

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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Upon Edn ligand binding endothelin receptors can
2021-01-25

Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example
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At the therapeutic level the logical
2021-01-25

At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn
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The DNA damage response DDR is
2021-01-25

The DNA damage response (DDR) is a cellular mechanism that protects against DNA damage induced by endogenous and exogenous factors, it includes changes in cellular processes such as ONC201 receptor regulation, DNA damage repair, apoptosis and chromatin remodeling. In recent years, the DDR has been
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In anticipation of an approach based
2021-01-23

In anticipation of an approach based on modification of the cyclohexylacetic DHEA subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1, although they
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The phenotypes of KD Ddr
2021-01-23

The phenotypes of KD-Ddr2 transgenic mice were less severe than expected from the results of miDdr2-transfected ATDC5 cells, which indicated that DDR2 might play important roles in endochondral ossification but neither critical nor essential roles in determining total body and skeleton size. The gr
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br Patients and methods br
2021-01-23

Patients and methods Results Table 1 shows relevant demographic and clinical characteristics of the 123 patients in the cohort. BAL fluid samples were obtained at a median of 172.5 days after allo-HSCT (range 3 days to five years). Discussion The definitive abandonment of traditional cult
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Therapeutic options targeting intrahepatic resistance are ve
2021-01-23

Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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Hinokitiol has versatile abilities as anticancer antimicrobi
2021-01-23

Hinokitiol has versatile abilities as anticancer, antimicrobial and molecule transport agents and appears to have no developmental toxicity or carcinogenic effects (Imai et al., 2006b). For anticancer activities, it causes apoptosis and epigallocatechin gallate arrest in many different types of can
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The role of ETB clearing receptors has been studied in
2021-01-23

The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous gsk-3 of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all other cell
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br Concluding remarks and prospective Cardiac proteinopathy
2021-01-23

Concluding remarks and prospective Cardiac proteinopathy, a more common disease condition and more frequent cause of cardiomyocyte decay than previously thought, is largely neglected and no effective therapy exists yet. Protein quality control and protein degradation via autophagy or the ubiquiti
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br Materials and Methods br Acknowledgements We thank the st
2021-01-23

Materials and Methods Acknowledgements We thank the staff of beamlines ID29 and ID30A-1 of the European Synchrotron Radiation Facility. This work was supported by, the Marie Curie Career Integration Grant (PCIG13-GA-2013-630755), the Israel Science Foundation (Grant 1383/17) and the Israeli Ca
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The thermal behavior of the
2021-01-22

The thermal behavior of the UV-sensitive nanocomposites was investigated by DSC before and after irradiation in an extended temperature range (from −40 to 250 °C). Fig. 4a shows the thermograms of the non-irradiated GNP-DNA/PDMS nanocomposites in comparison with a neat PDMS sample. The filler-loaded
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Our data show a site specific interaction of DDR with
2021-01-22

Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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It is important to note that CRF may
2021-01-22

It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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