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TKI discontinuation studies demonstrate that a portion of
2020-02-24
TKI discontinuation studies demonstrate that a portion of TKI-treated CML patients remain in remission for up to 3 years, although long-term risk assessment is still necessary (Bansal and Radich, 2016). The majority of CML patients depend on lifetime TKI treatment, and substantial efforts have been
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In vitro studies suggest that cPLA does
2020-02-24
In vitro studies suggest that cPLA2α does not show clear preference for the headgroup present at the sn-3 position, although a slight preference for zwitterionic phospholipids such as PC and PE has recently been pointed out [24]. In this regard, mass spectrometry analyses of glycerophospholipid hydr
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Compared to ET all agonists
2020-02-24
Compared to ET-1, all agonists tested showed a 2–4 fold bias for the G protein constrictor assay compared to the β-arrestin assay (Table 1). This preliminary analysis indicated that at least modest pathway bias for endogenous ET peptides is possible, however the physiological significance of this, i
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There is evidence that the response
2020-02-24
There is evidence that the response of CYP450 activity to DEX is species-specific. CYP1A and CYP3A expressions were strongly induced by DEX in porcine hepatocytes (Rasmussen et al., 2014) and in rat and human, but not minipig or beagle dog hepatocytes (Lu and Li, 2001). Within fish, there are also s
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We also found downregulation of TRIM in the
2020-02-24
We also found downregulation of TRIM32 in the hearts of dilated and hypertrophic cardiomyopathy patients in addition to TAC and phenylephrine treated mice [51]. TRIM32 and Dysbindin are known to interact in skeletal muscle, and we could confirm this interaction in cardiomyocytes as well. In cardiomy
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On the basis of the
2020-02-24
On the basis of the published articles, it is known that chemokines are produced by leukocytes and tissue cells, constitutively or after induction. Chemokines are responsible for the recruitment of leukocytes to maintain proper functioning of the immune system [14]. They exist in the central nervous
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In the present study promoting bile acid
2020-02-24
In the present study, promoting bile N-acetyl D-galactosamine synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for li
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A different example of substrate dependent activation is see
2020-02-22
A different example of substrate-dependent activation is seen in CSN5, a JAMM-type DUB found in the eight subunit COP9 signalosome (CSN) [34]. The CSN deconjugates NEDD8 (neural precursor cell expressed developmentally downregulated 8) from Cullin Ring ubiquitin E3 ligases (CRLs). Through this activ
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ApicomplexansApicomplexans are unicellular and spore forming
2020-02-22
ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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Substitutions on the benzene ring
2020-02-22
Substitutions on the benzene ring of the phenyl acetic valsartan and alcohol mg 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
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A widely accepted mechanism to differentiate hESCs
2020-02-22
A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the nitric oxide booster [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is pivota
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A particularly important system in which
2020-02-22
A particularly important system in which Eph-ephrin signaling has been widely studied is neural development, in which downstream signal transduction controls neural stem cell (NSC) proliferation, migration, and survival both during early development and in adulthood (19, 20, 21). Furthermore, Eph-ep
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Two GPCR subtypes of interest in the myocardium are
2020-02-22
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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br Localization of D receptors
2020-02-22
Localization of D2 receptors in striatum One characteristic of D2Rs that has complicated their study is their expression in multiple neuronal populations within striatum, both pre- and postsynaptically (Beaulieu and Gainetdinov, 2011). In addition to spiny projection neurons (SPNs), which are the
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Here we report for the
2020-02-21
Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a
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