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Subcellular domains where Rac is active show
2022-02-08

Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho
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siRNA construction and transfection For small interfering RN
2022-02-08

siRNA construction and transfection. For small interfering RNA (siRNA) experiments, we used Stealth™ select RNAi oligonucleotides targeted against GPR120 (Gibco/Invitrogen). The target sequence of siGPR120 used were; sense 5′-AAGUGGGUGCGAUUGACUUGGUCCA-3′ and antisense 5′-UGGACCAAGUCAAUCGCACCCACUU-3′
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We first set out to identify the minimum pharmacophore
2022-02-08

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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br FXR Agonists Azepinol b
2022-02-07

FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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Tamoxifen is still the most
2022-02-07

Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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BAN ORL 24 mg An increased sympathetic tone and the hormone
2022-02-07

An increased sympathetic tone and the hormone glucagon are the main glucose mobilizing factors [28], [29]. Single-cell transcriptome analysis of human islet cells suggests the expression of Ffar1 not only in β-cells but also in α-cells [30]. Moreover, analysis of rat α-cells indicates that FFAR1 exp
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The previous studies focused on the
2022-02-07

The previous studies focused on the regulation of GK activity by nutrients directly or nutritional hormones (Panserat et al., 2014), there was still a lack of studies paid attention to GK both in activity level and transcriptional level. Besides, the GK regulation by dietary src kinase inhibitor has
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br Vertebrate steroid receptor evolution
2022-02-07

Vertebrate steroid receptor evolution Conclusion The teleost WGD event resulted in the duplication of the vertebrate GR and MR and two GRs have been retained in the majority of teleost fish studied so far. The molecular basis for this retention has yet to be fully understood. The cloning of th
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In summary this study demonstrated the cDNA cloning and char
2022-02-07

In summary, this study demonstrated the cDNA cloning and characterization of the galanin type II receptor (GalR2) and a novel GalR2-like receptor (GalR2-L) in chickens, in which these two receptors are possibly originated from a gene 96 7 receptor event that occurred in the early vertebrate lineage
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Isoflurane administration during i t procedures
2022-02-07

Isoflurane administration during i.t. procedures can complicate the interpretation of our results since isoflurane has been shown to have both neuroprotective and neurotoxic effects (Jiang et al., 2017). Isoflurane pretreatment has been implicated as having protective effects in ischemia in animal m
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After initial optimization of the distances
2022-02-07

After initial optimization of the distances we obtained the structure iG shown schematically in Fig. 1. This is the telomeric fragment of chromosome with the noncanonical structures of i-motif and G-quadruplex placed symmetrically in the middle of the duplex. Obviously, we consider the situation whe
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br Acknowledgements This study was supported by National Ins
2022-02-07

Acknowledgements This study was supported by National Institutes of Health grant (R01GM104037), VA grant (BX002741), and Rutgers Busch grant. Nuclear receptor FXR is the master regulator of bile acids homeostasis The farnesoid X receptor (FXR) belongs to a family of proteins known as nuclear
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Natural product based drug discovery can be enhanced with
2022-02-07

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in 960 8 binding assays, we used molecular modeling to predict how well these compounds fit th
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Previous research has suggested that differences in spatiote
2022-02-07

Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, lac
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Now we turn to the other channel
2022-02-07

Now we turn to the other channel through which the risk-taking incentives provided by option compensation affect corporate debt maturity. Jensen and Meckling (1976) argue that the payoff structure of debt holders in a levered firm is concave, while that of equity holders is convex, thus, shareholder
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