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With the identification of small
2021-10-21

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy
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br STAR Methods br Acknowledgments We thank Prof Y
2021-10-21

STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a
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rifampicin Several studies have proposed that high
2021-10-20

Several studies have proposed that high levels of KYNA in the rifampicin contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizophreni
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It has been reported that aberrant GPR
2021-10-20

It has been reported that aberrant GPR120 expressions were detected in colorectal carcinomas, compared with normal tissues. In addition, GPR120 stimulated cell motile activity and angiogenic property in colon cancer cells [10]. Recently, we indicated that GPR40 suppressed cell motile and invasive ac
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br Acknowledgments br The study was funded by the
2021-10-20

Acknowledgments The study was funded by the European Commission FP7-project Beta-JUDO (Grant 279153), and Swedish Diabetes Association (Grant DIA 2013-043) and Family Ernfors Foundation (Grant 150430). Free fatty EW-7197 receptor receptors (FFARs) represent a family of G-protein coupled rec
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br Experimental section br Results and
2021-10-20

Experimental section Results and discussion Conclusion The evaluation of the inhibitory potential of these derivatives towards eight kinases showed that the brominated hybrids (3k) and (3l) are the most active against the PIM1 and CLK1 kinases. The methylation of the nitrogen MDV3100 of the
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A second feature of the Ras type GTPases is
2021-10-20

A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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The isoenzyme hGSTP is an attractive drug target due
2021-10-20

The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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FOLE was recently approved for
2021-10-20

FOLE was recently approved for use in PN-dependent patients in the United States. However, potential adverse effects of FOLE, including bleeding risk, and effects on the immune system [8], [39], render its use in certain patient populations controversial. Identification of key downstream modulators
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DNA repair is essential for cell survival and for tissue
2021-10-20

DNA repair is essential for cell survival and for tissue homeostasis given that cellular DNA is constantly challenged by various endogenous and exogenous genotoxic factors that generate DNA damage: structural and chemical modifications of a primary DNA sequence. Various organisms have evolved multip
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Due to the requirement of high end methods
2021-10-20

Due to the requirement of high-end methods such as total internal reflection fluorescence (TIRF) microscopy to visualize lipid rafts, isolation procedures are employed to study the protein content of lipid rafts [29]. The different methods utilized to isolated lipid rafts and other low density micro
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Regarding the causative diseases of ES patients
2021-10-20

Regarding the causative diseases of ES, patients with unknown cause and those with encephalitis had significantly higher CSF levels of UNC669 against GluN2B-NT2 and GluN2B-CT than the disease controls, but patients with genetic disorder and those with cortical dysplasia showed no significant differ
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L Family Leguminosae widely distributed
2021-10-19

L. (Family Leguminosae) widely distributed in tropical and subtropical regions of the world. As a medicinal and edible plant, it is widely used in Asia, especially in China, Korea, Japan and India. It was first recorded in Shen Nong Ben Cao Jing (神农本草经), and was described having the effect of cleari
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The first GSM was identified from the
2021-10-19

The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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To obviate the mitogenic FGF activity
2021-10-19

To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino
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