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Overall we found that all hormone
2020-08-10

Overall, we found that all hormone treatment groups were able to learn spatial working and reference memory tasks, as shown by their performance across days on the WRAM (days 2–12, collapsed across the 4 trials) and the MWM (days 1–5, collapsed across the 4 trials). During the acquisition phase of t
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br Roles of ERR in Physiology and Disease
2020-08-10

Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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br Structure and function of EPAC
2020-08-10

Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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Grapiprant is a selective antagonist for
2020-08-10

Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Our present results support a major role of EP
2020-08-10

Our present results support a major role of EP1 receptors in peripheral heat sensitization and a smaller contribution to central heat sensitization but no contribution to mechanical sensitization. While the contribution of peripheral EP1 receptors to heat hyperalgesia is in good agreement with the a
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The present study showed evidence that
2020-08-10

The present study showed evidence that the AT1 and the ETA receptors were not expressed near or on the plasma membrane as monomers, but also as possibly constitutive dimers and tetramers. For both receptors, the proportion of monomers, dimers and tetramers were unaffected by their respective agonist
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The development of novel approaches
2020-08-10

The development of novel approaches to study GPCR-mediated transactivation in live poly ic is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Grb2 t
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Our study provides proof of principle for
2020-08-10

Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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Dose response analysis Fig can be
2020-08-08

Dose response analysis (Fig. 2) can be performed on AZD3264 receptor in culture, in tissue, in animals or even in patients. Many different responses can be measured, including mRNA levels, reporter gene activity, gene product (e.g. enzyme) activity or even physiological functions such as inhibition
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In this study we make
2020-08-08

In this study we make the novel observation that villin-1 and gelsolin are down-regulated in response to diverse cellular stressors, including bacteria associated with the pathogenesis of CD. The high plasticity and dynamics of the Santacruzamate A mg cytoskeleton are exploited by bacterial and vir
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As mentioned above EBI and its ligand show some similarities
2020-08-08

As mentioned above, EBI2 and its ligand show some similarities to the sphingosine 1-phosphate (S1P)/S1P-receptor system, which mediates T cell egress from lymph nodes. Blockade of this system yielded in the first oral drug for MS patients named fingolimod. Therefore, the hope that EBI2 deficiency wo
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CSN is a conserved typically eight subunit multiprotein comp
2020-08-08

CSN is a conserved, (typically) eight subunit multiprotein complex composed of six PCI (proteasome lid, CSN, mk 801 australia factor 3) subunits (CSN1–CSN4, CSN7 and CSN8) and two MPN (MPR1/PAD1 amino-terminal) domain-containing subunits (CSN5 and CSN6). Cullin deneddylation is specifically mediate
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Another interesting finding regarding substrate
2020-08-06

Another interesting finding regarding substrate selectivity of iPLA2-VIA in whole cellular systems stems from the observation that some of the major species hydrolyzed by the enzyme contain a 16:1 fatty norepinephrine bitartrate at the sn-2 position [57,119], raising the possibility that iPLA2-VIA m
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Proteases as multifunctional enzymes play
2020-08-06

Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on.
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SB273005 Due to intense biological alterations induced by va
2020-08-06

Due to intense biological alterations induced by various risk factors of obesity, the adipose tissue undergoes adaptations such as adipocyte hypertrophy superimposed with hyperplasia (Jo et al., 2009). In addition to these changes, the adipocytes experience a process of cellular differentiation ther
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