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In different body organs a number of biological functions ar
2020-07-09
In different body organs, a number of biological functions are generally mediated by binding of the extracellular substances to the particular transmembrane receptors, which results in subsequent signal stimulation by intracellular signaling cascades. These cascades function over the complex network
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As for the molecular mechanism
2020-07-09
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of elvitegravir with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with high EphB4 expression le
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To study systemic potential of the selected
2020-07-09
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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br Results br Discussion In this paper
2020-07-09
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 VX-689 via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhibito
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ELUXA HM EMSI is an ongoing
2020-07-09
ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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Pifithrin-μ br Acknowledgments This work was supported by Gr
2020-07-09
Acknowledgments This work was supported by Grants from the National Research Foundation (2010-0000782) and the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquityl
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br Conclusion In the last year
2020-07-09
Conclusion In the last year, significant advances in our understanding of ubiquitin transfer by IAPs and related E3 ligases have been made. The three crystal structures of the RING-bound E2~Ub show that the conjugate is bound by the RING domain in the closed conformation, where the I44-centered f
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A939572 In our recent study we established a procedure
2020-07-09
In our recent study, we established a procedure to examine the chromatin binding of XRCC4 using a biochemical fractionation analysis using a detergent Nonidet P-40 [22]. In this study, we investigated the role of LIG4 and its subdomains in the recruitment of XRCC4/LIG4 complex to chromatin. Mater
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wst-1 br Results and discussion In the present study we
2020-07-09
Results and discussion In the present study, we used a set of compounds (Fig. 2) consisting of ATP (a), dATP (b), an ATP analog containing β,γ-nonhydrolyzable hypophosphate P-P bond (c), and three pairs of P-diastereoisomers of α-thio-ATP analogs (d,e,f) containing a sulfur wst-1 instead of one
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br Acknowledgements We thank Dr Tai
2020-07-09
Acknowledgements We thank Dr. Tai-Yuan Yu and Miss Chun-Ping Chang for helping with the drug/DNA sequence specificity study. We also thank the Chemical Synthesis Core and the Pathology Core Laboratory of IBMS for synthesizing SL-1 and for performing the pathology analysis, respectively, and the T
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DDR plays a crucial role in
2020-07-09
DDR2 plays a crucial role in regulating a wide variety of fundamental cellular processes, including cell proliferation, differentiation, and adhesion [17], [28], [29], [30]. The authors revealed compromised cell migration in DDR2-silenced fibroblasts exposed to Ang II, most likely due to the loss of
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The focus of this review is on the diacylglycerol acyltransf
2020-07-08
The focus of this review is on the diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) enzymes, DGAT1 and DGAT2, that catalyze the esterification of a fatty acyl moiety to a DAG molecule to produce TAG. These enzymes commit DAG to being stored as TAG rather than being diverted for the synthesis of ph
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Moreover a ligand for fusin has
2020-07-08
Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO Adenosine-5\'-diphosphate receptor transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, ha
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Besides the enhanced expression of costimulatory and adhesio
2020-07-08
Besides the enhanced expression of costimulatory and adhesion proteins, also the expression of the CD83 surface molecule is strongly enhanced during DC maturation (Banchereau and Steinman 1998; Banchereau et al. 2000). In fact, CD83 is a major cell surface marker for fully mature DC, as it can not b
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Regarding the mechanism of action of
2020-07-08
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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