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bcr-abl tyrosine kinase inhibitors br Fragment based drug di
2020-02-27
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical bcr-abl tyrosine kinase inhibitors space with libraries which are smaller in size, producing drug leads with high ligand
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Introduction Cyclin dependent kinases CDKs are a
2020-02-27
Introduction Cyclin dependent kinases (CDKs) are a family of proline-directed serine/threonine kinases with roles in regulation of crucial cellular processes such as AR-42 HDAC and transcription [1]. One of the unifying features of this family is its dependence on association with cyclins/cyclin-l
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br Discussion In depression an
2020-02-27
Discussion In depression, an activation of the inflammation process and production of cytokines (including chemotactic cytokines – chemokines) and their receptors may occur due to the stimulation of the immune system. One of the earliest studied and described cytokines in depression is interleuki
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Intriguingly one E residue may serve
2020-02-26
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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br Results and Discussion br Experimental
2020-02-26
Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac
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Upstream Stimulatory Factor USF binding to the
2020-02-26
Upstream Stimulatory Factor (USF) binding to the −65 E-box is required for the regulation of FAS promoter activity in fasting/feeding [97], [98]. DNA-PK are identified as a USF-interacting protein [99]. In response to feeding/insulin, the transient double-stranded DNA breaks occurred during the tran
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The possibility that a carboxyl group attached to the
2020-02-26
The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a
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ac 723 In the present study we combined activity based
2020-02-26
In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis ac 723 and leaves, we demonstrate that this sub-class of plant proteases is activated in respo
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Introduction The Bromeliaceae family is
2020-02-26
Introduction The Bromeliaceae family is one of the most morphologically and ecologically diverse flowering plant families native to the tropics and subtropics of the New World (Benzing, 2000). They comprise >3000 species and are traditionally divided into three subfamilies: Pitcairnioideae, Bromeli
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In summary our findings show that LPS can
2020-02-26
In summary, our findings show that LPS can activate CysLT2R on microglial signaling to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of LPS-
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By using the C elegans Matrisome
2020-02-26
By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome OR-486 sale in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elegans matrisome for var
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br Experimental Procedures br Author Contributions M M and
2020-02-26
Experimental Procedures Author Contributions M.M. and M.T. designed and supervised the study. S.I. conducted the analysis on NOG-rd mice. H.-Y.T., M.F., and T.M. conducted and analyzed MEA. S.I., H.-Y.T., and M.M. performed 3D image analysis. N.K., T.K., M.G., and R.T. planned and established
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MSCs are self renewing multipotent progenitor
2020-02-26
MSCs are self-renewing, multipotent progenitor cells, with multilineage potential to differentiate into adipocytes, osteocytes, and chondrocytes. In addition, MSCs can migrate to sites of inflammation, supporting hematopoiesis and homeostatic maintenance. Given their unique therapeutic properties, M
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Recently roflumilast has been approved as the first selectiv
2020-02-26
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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PGE EP activation has been
2020-02-26
PGE2-EP4 activation has been found to attenuate the activation of microglia and to prevent lipid peroxidation and pro-inflammatory gene expression in a murine model of lipopolysaccharide (LPS)-induced butein sale inflammation [15]. Moreover, PGE2/EP4 signaling has elicited a protective function in
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