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Compound was prepared from chloroindole by acylation
2019-10-10
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole 11-dUTP derivative (). Derivatives and were pre
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In conclusion we designed novel E inhibitors based on
2019-10-10
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and , we f
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It is well established that
2019-10-09
It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed
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The anticholinesterase activities of all subfractions derive
2019-10-09
The anticholinesterase activities of all subfractions derived from EtOAc extract were detected and summarized in . Fraction 5 and its resulting subfractions (5B, 5C, 5D, 5C3, 5C4, 5D3, and 5D4) were found to show attractive activities. Subsequently, ten compounds (–) were obtained from these active
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During the entire life of individual articular chondrocyte
2019-10-09
During the entire life of individual, articular chondrocyte as well as subchondral bone receives acute or chronic stress. Joints homeostasis is maintained by biomechanical stress, as rapid loss of proteoglycan in joints occurs due to immobilization or disuse. These osteophytes are fibrocartilage cap
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br Experimental Procedures br Author
2019-10-09
Experimental Procedures Author Contributions M.B., with input and help from T.T.H., conceived the project, designed and performed the experiments, analyzed the data, and wrote the manuscript. B.B.B. and F.D.M. synthesized the wild-type and (nonhydrolyzable, NH) Ub tetramers and contributed Fig
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Here we explored the relative contribution of D like
2019-10-09
Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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SR3335 kinase The other interesting observation made
2019-10-09
The other interesting observation made during this study relates to the differences between the discrete IR-induced γH2AX foci and the robust H2AX phosphorylation observed during apoptotic DNA fragmentation. The pattern of H2AX phosphorylation observed during DNA fragmentation possibly reflects the
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br Synthesis and mechanism of fluorescent
2019-10-09
Synthesis and mechanism of fluorescent DNA-CuNMs Application of fluorescent DNA-CuNMs Summary and conclusions In summary, we introduce recent research progress in the synthesis and various applications of DNA-CuNMs. DNA-CuNMs with novel catalytic, electrical and optical properties can be ob
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br Introduction Pattern separation is the ability to make
2019-10-09
Introduction Pattern separation is the ability to make distinct representations from highly overlapping information, a process which is important for memory encoding (Clelland et al., 2009). For correct pattern separation, old information needs to be retrieved and compared to new information. If
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br Materials and Methods br Acknowledgements br Introduction
2019-10-09
Materials and Methods Acknowledgements Introduction The extracellular matrix (ECM) is a dynamic structure that acts as a scaffold for the mechanical support of multicellular organisms. It is responsible for the organisation of different tissues and regulates critical events in development a
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br Experimental Procedures br Author Contributions M M and M
2019-10-08
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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br APC C Uses a Dynamic Cullin RING
2019-10-08
APC/C Uses a Dynamic Cullin–RING Mechanism to Elongate Polyubiquitin Chains Human APC/C generates Lys11-linked poly-Ub chains through an entirely different mechanism, via the distinctive E2 enzyme, UBE2S 30, 31, 32. Although APC2 and APC11 are necessary and sufficient to activate UBE2S, the mecha
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MicroRNA miRNA is a class of highly conserved non
2019-10-08
MicroRNA (miRNA) is a class of highly conserved, non-coding small molecules containing 19–25 nucleotides. miRNAs are involved in the regulation of genes associated with cancer development and progression and therefore can act as oncogenes, by contributing to tumor formation,17, 18 or as tumor suppre
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Programmed cellular death or apoptosis is a
2019-10-08
Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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