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br STAR Methods br Acknowledgments We thank
2020-09-19

STAR★Methods Acknowledgments We thank members of R.L. lab and F. Schweisguth for critical reading of the manuscript. We are also grateful to F. Janody, M. Miura, C. Bökel, H.D. Ryoo, G. Jiménez, the Bloomington Drosophila Stock Center, the Drosophila Genetic Resource Center, the Vienna Drosoph
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The reduction of the calcium response to AVP
2020-09-19

The reduction of the calcium response to AVP could be also due to a PKA-mediated effect of desensitization of IP3R, as described in rat megakaryocytes [41]. Furthermore, PKA activation inhibits intracellular Ca release in mouse pancreatic acinar cells [42] or in rat cerebellum [43]. The phosphorylat
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br Declaration of conflicting interests br Funding The autho
2020-09-19

Declaration of conflicting interests Funding The author(s) disclosed receipt of the following financial support for the research, authorship, and/or publication of this article: This work was supported by CT Stem Cell grant # 15-RMB-YALE-07 (to L.E.N), and by an unrestricted Research Gift from
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KN-92 phosphate While previously reported optimizations on
2020-09-19

While previously reported optimizations on KN-92 phosphate focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore
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br Materials and methods br Results br Discussion
2020-09-19

Materials and methods Results Discussion The EP4 Griseofulvin synthesis for PGE2 is similar to the EP1, EP2 and EP3 receptors in that they all have seven transmembrane segments and are coupled to Gα subunits of heterotrimeric G proteins, with a different Gα subunit for each receptor (Sugimo
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br Introduction Prostaglandin E PGE signals through separate
2020-09-19

Introduction Prostaglandin E2 (PGE2) signals through 4 separate G-protein coupled receptor sub-types (EP1, EP2, EP3 and EP4) to elicit a variety of physiological and pathophysiologic effects. EP2 and EP4 increase cAMP levels in the cell via adenylate cyclase activation, whereas EP3 inhibits cAMP
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Enzyme activity loss during the hydrolysis
2020-09-19

Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important
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Dual inhibition of ACE and NEP as a strategy
2020-09-19

Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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dihydroquercetin mg During the host response to inflammation
2020-09-18

During the host response to inflammation, inflammatory mediators, including release of pro-inflammatory cytokines, have been associated with altered content, expression, and activity of CYP450 enzymes, consequently leading to alterations in the metabolism and elimination of certain drugs. The losses
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Proinflammatory cytokines induce ER stress in many
2020-09-18

Proinflammatory cytokines induce ER stress in many mammalian cell systems.32, 33, 34 Our results demonstrate that these cytokines also trigger ER stress in trophoblast JEG-3 cells. However, the severity of stress is likely low grade because only the PERK-EIF2A arm of the UPRER pathway was activated.
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Results of the present study demonstrate
2020-09-18

Results of the present study demonstrate that 25-OHC treatment of THP-1 monocytes induced vimentin intermediate filament reorganization to more cortical structures and a polarized phenotype (Fig. 5). Vimentin is the major intermediate filament protein present in leukocytes and plays an important rol
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In addition to playing important roles
2020-09-18

In addition to playing important roles in the immune system, EBI2 is also expressed in the Sennoside C of the central nervous system (CNS), namely astrocytes, and this receptor regulates astrocyte signalling, as well as astrocyte cell migration (Rutkowska et al., 2015, Rutkowska et al., 2016a). Mor
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AZD3514 Programmed cellular death or apoptosis
2020-09-18

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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br Results and Discussion br Conclusions
2020-09-18

Results and Discussion Conclusions Understanding the connections between function and fitness is a primary goal of many biological disciplines including systems biology and molecular evolution. While sound approaches have been developed to understand the connections between function and fitnes
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br Future perspectives Understanding how peptides are
2020-09-18

Future perspectives Understanding how peptides are degraded, particularly those which may be therapeutically useful, such as GLP-1, has proved to be invaluable in providing a rationale for the development of a novel class of therapeutic agents. However, while DPP-4 plays an important role in the
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