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During the past decade it became
2020-09-17
During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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The underlying mechanisms of how
2020-09-17
The underlying mechanisms of how progesterone prolongs pregnancy, although not completely understood, are thought to have to do with reduction in uterine contractility, antimicrobial protein up-regulation, immunosuppression, and inflammatory inhibition. Specific to preterm PROM, progesterone has bee
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Given that dimethylamine substitution was tolerated as in SR
2020-09-17
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated 4a 5 2 3.25 a synthesis amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR
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The transcription factor CREB has been extensively
2020-09-17
The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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An important focus of the present study has been
2020-09-17
An important focus of the present study has been the interaction of HUVECs with extracellular matrix in the regulation of angiogenesis. Matrigel is a gelatinous protein extract secreted by Engelbreth–Holm–Swarm mouse sarcoma cells, and is considered to be a good model of the extracellular matrix (Kl
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Previously we have reported that magnitude of the
2020-09-17
Previously, we have reported that magnitude of the disruption of the blood–aqueous barrier after paracentesis was reduced by 82% in EP4 receptor knockout mice (Biswas et al., 2006). In the present study, we observed that pretreatment of EP1 receptor knockout mice with EP4 receptor antagonist, reduce
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br Materials and methods br
2020-09-17
Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic 96 7 induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to enter status epileptic
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Omar Farha and coworkers have
2020-09-17
Omar Farha and coworkers have recently successfully employed metal-organic frameworks (MOFs) to tackle these limitations while retaining the essential characteristics of an immobilization material. MOFs consist of metal ions, or small clusters thereof, coordinated with organic ligands. MOFs are hig
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br Clinical potential of ET receptor biased
2020-09-16
Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]
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Gene chip is a detection technique that can detect
2020-09-16
Gene chip is a detection technique that can detect all the time-point differentially expressed genes (DEGs) information within the same sample. However, due to sample heterogeneity or different sequencing platform, the results for the expressed mRNAs are inconsistent with different gene profile. The
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Moving forward the new mathematical model opens doors for un
2020-09-16
Moving forward, the new mathematical model opens doors for understanding the SCF network, where activity of a component is blunted through mutation or altered in expression in diseased states, and during therapeutic intervention. Computational modeling could reveal underappreciated secondary or tert
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We propose two different pathways
2020-09-16
We propose two different pathways for the production of this species: either that described by Dooley [24], where the phenol ring is first activated by binding of its oxygen to copper, or one where a copper-peroxo species would directly react with an active site tyrosine residue (Scheme 1B). This se
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br Materials and methods br Results br Discussion
2020-09-16
Materials and methods Results Discussion The present study shows that 1) overexpression of wild-type or mutant α-SYN interferes with forskolin-induced DBH up-regulation, 2) α-SYN enters into the nucleus and is able to bind to CRE region, compete for CREB, and attenuate CRE-mediated transcri
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The human serotonin hydroxytryptamine HT receptor family con
2020-09-16
The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per
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Introduction Double strand break DSB is
2020-09-16
Introduction Double strand break (DSB) is the most deleterious damage that threats DNA integrity. This frequent damage arises from environmental stress like UV, chemical agents or ionizing radiations (IRs). Although environmental stress does not lead directly to DSB, it produces CORM-3 damage, mut
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