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Our previous high throughput screening HTS
2021-07-19

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Cy3 NHS ester (non-sulfonated) assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [
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Acidosis has lethal consequences but alkalosis due to
2021-07-19

Acidosis has lethal consequences, but alkalosis (due to chloride depletion, potassium depletion, and excess mineralocorticoid) is not tolerated as well (Luke and Galla, 2012). In this regard, efforts to restore pH to normal physiological level, in the most benign way should be the goal of researcher
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Prote br Acknowledgments br Introduction Hypertensive retino
2021-07-19

Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat
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Impaired dopaminergic systems associated with MA have been w
2021-07-17

Impaired dopaminergic systems associated with MA have been well-documented (Walsh and Wagner, 1992, Kim et al., 1999, Nakajima et al., 2004, Shin et al., 2012, Shin et al., 2017b, Dang et al., 2016, Dang et al., 2017b). Previous reports have suggested that early MA use may be linked to higher risk f
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Collagen compaction and alignment are generated by cell medi
2021-07-17

Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano
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Many investigators participated in the studies
2021-07-17

Many investigators participated in the studies on the regulation of the LRRK2-IN-1 and experiments indicated that the process was conserved across many eukaryotic species including humans [127]. Because cancer cells exhibit dysregulated cell division along with the presence of abnormal chromosome nu
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Previously published results on this topic are inconsistent
2021-07-17

Previously published results on this topic are inconsistent. Stressin1-A, a novel CRF1 receptor agonist, increased anxiety-like behavior in the social interaction and shock-probe tests [51]. Pharmacological blockade of CRF1 (NBI-30775) reversed both CRF-induced increases in startle and CRF-induced d
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br Introduction The dorsal periaqueductal gray matter
2021-07-17

Introduction The dorsal periaqueductal gray matter (dPAG) is a midbrain site markedly involved in fear/anxiety-evoked responses as well as in nociception (see, for example, Bandler and Carrive, 1988, Deakin and Graeff, 1991, Fardin et al., 1984a, Fardin et al., 1984b, Litvin et al., 2007). Chemic
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Introduction The carnitine choline acyltransferase family is
2021-07-17

Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) Bedaquiline and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this family consists of se
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Further studies are needed as continuation of
2021-07-17

Further studies are needed as continuation of this work to explore the effects of type and position of substituents of pyridazinone ring on anti-inflammatory activity profile. Taking into consideration that the phenyl moiety at position 2 wasn't a favorable substituent, even certain studies may be r
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Astrocytes play a key role in the
2021-07-16

Astrocytes play a key role in the brain, as these cells are involved in fluid, ion, pH, and neurotransmitter homeostasis, synapse function, energy and metabolism and blood-brain barrier (BBB) maintenance (Sofroniew and Vinters, 2010). PA is able to activate different damaging responses in astrocytes
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We next turned our attention to the position
2021-07-16

We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a
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Gene chip is a detection technique that can detect
2021-07-16

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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Our data furthermore suggest that Ch h
2021-07-16

Our data furthermore suggest that Ch25h-induced oxysterols could play an important role in modulating the immune cell migration. Mechanistically, we observed impaired trafficking of CD44+CD4+ T cells in mice deficient for Ch25h. CD44+CD4+ T cells lacking EBI2, the receptor of 7α-25OHC, were delayed
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br Expression data suggest involvement
2021-07-16

Expression data suggest involvement of additional TRIMs in heart function Given the complexity of the cardiac function, involved molecular pathways and processes, and the fact that only a few of the TRIMs have thus far been shown to have a cardiac role, we hypothesized that there would be more TR
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