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Furan analogs and N methylpyrrole analogs had
2020-03-16

Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 bosentan affinity and an increased antagonist activity, while the corresponding chemical modifica
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It is noteworthy that little is known as to the
2020-03-16

It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti
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br Introduction The identification of genetic
2020-03-16

Introduction The identification of genetic variants that influence susceptibility to Parkinson\'s disease (PD) determines functional studies, the generation of model systems and directs therapeutic strategies. To date, classical candidate gene association studies and genome-wide approaches have f
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br Experimental Procedures br Acknowledgments
2020-03-16

Experimental Procedures Acknowledgments The authors wish to thank P. Costet (University of Bordeaux) and Véronique Guyonnet-Duperat (FR TransBioMed, Plateforme de Vectorologie, University of Bordeaux) and Prof. Nils-Göran Larsson and Dr. Bettina Bertalan (Max Planck Institute for Biology of Ag
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SB203580 From the general synthetic route we first synthesiz
2020-03-16

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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Substitutions on the benzene ring of
2020-03-16

Substitutions on the benzene ring of the phenyl acetic p2y inhibitor moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryl
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Three new trans P Hs
2020-03-16

Three new trans-P4Hs (AlP4H, MiP4H and ScP4H) discovered by a genome mining approach in this study were all located in branch A containing DaP4H sequence. Although another three candidates from Amycolatopsis mediterranei, Bradyrhizobium sp. ORS285 and O. indicum were successfully expressed as solubl
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br Introduction Receptor tyrosine kinases RTKs are criticall
2020-03-16

Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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Docking experiments showed that Me MeGlcA
2020-03-16

Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same Parthenolide and no new interactions were observed
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TgTCEA from petals TgTCEA and TgTCEB from pollen grains
2020-03-16

TgTCEA from petals (TgTCEA1) and TgTCEB from pollen grains (TgTCEB1) were used throughout the study. The recombinant enzymes were expressed in , and purified as the His-tag-free forms as described previously., Enzyme reactions were performed at 4 mM substrates under the same conditions as described
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In view of the hypotensive effect of
2020-03-16

In view of the hypotensive effect of endothelial-specific overexpression of eNOS [17], [19], [28] we correlated skeletal muscle eNOS expression with sBP including data on colony 5 of eNOS-Tg [17] which was used to generate eNOS-Tg/KO (Fig. 4D). We found a highly significant one phase exponential dec
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br Introduction Cancer related inflammation is associated wi
2020-03-13

Introduction Cancer related inflammation is associated with poor prognosis and reduced survival in numerous human malignancies. Expansion of myeloid derived immune Cyanine 3-dUTP in response to tumor-secreted factors largely contributes to the heightened systemic and intra-tumoral inflammatory m
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br Results and Discussion br Experimental Procedures br
2020-03-13

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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In a study carried out by Aunis et
2020-03-13

In a study carried out by Aunis et al. the properties of soluble DBH and membrane bound were examined [23]. The membrane bound enzyme was shown in mm hcl to the soluble form to have thermal denaturation at higher temperatures of 43.5–44°C. Similar discontinuities in the Arrhenius plots were obtaine
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Several limitations of this study need to
2020-03-13

Several limitations of this study need to be acknowledged. First, although 200 patients were recruited into this study and completed assessments at baseline, only 89 patients completed the cognitive tests after 8weeks of treatment. The relatively long study period (8weeks) was the main reason for th
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