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In summary the SAR of a series of phenylpropanoic acid
2021-12-24
In summary, the SAR of a series of phenylpropanoic acid-free fatty I-BET151 receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficacy
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To evaluate the role of increased FPPS expression
2021-12-24
To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on LDC1267 progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cells (A and B), h
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In our cohort each patient had a median of
2021-12-24
In our cohort, each patient had a median of 2 Anti-FXa measurements performed daily and a median of 1 infusion rate change daily to maintain therapeutic unfractionated heparin levels. Previously, several studies have documented that APTT-based protocols lead to more fluctuations in comparison with A
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br Acknowledgments Work in SI
2021-12-24
Acknowledgments Work in SI’s laboratory is supported by grant IM 20/4-1 from the Deutsche Forschungsgemeinschaft, Bonn (Germany) and grant EKFS 2012_A309 from the Else Kröner Fresenius Stiftung, Bad Homburg (Germany). FW’s group is supported by the Dr Vaillant Foundation and the Dutch Burns Found
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Next to their indirect effect on
2021-12-24
Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more
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Yeast two hybrid screening studies have
2021-12-24
Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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br Role of BKCa in Cardiovascular System br Perspective for
2021-12-24
Role of BKCa in Cardiovascular System Perspective for BKCa Channels as Potential Target for Cardiovascular Diseases The intermediate conductance Ca-activated K+ channels (IKCa; KCa3.1, also known as SK4, IK, IKCa1, SMIK) were first discovered in erythrocytes by Gardos (1958) and then also fo
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Optimization of the tetrahydroindazole series
2021-12-24
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ().
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An advantage of photolabeling with tritiated photoprobes fol
2021-12-23
An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled maprotiline and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with other
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A general synthesis of the tetrazole is shown in First
2021-12-23
A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic gw web followed by reduction of the aldeh
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Next we conducted subgroup analyses with stratification alon
2021-12-23
Next, we conducted subgroup analyses with stratification along interaction variables, namely the PPARG SNP and fasting NEFA. The study population was thus stratified into high and low NEFA (along the median NEFA, 561 μmol/L), and PPARG minor allele (Ala) carriers. This stratification resulted in 4 s
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Mammals and birds are sensitive either to
2021-12-23
Mammals and birds are sensitive either to hypo or hyper glycemia. In contrary some frogs when freezing/thawing experience very high glycemia (Storey and Storey, 1986). Nevertheless when the effect of temperature on Fru-2,6P2 concentration was investigated, the constant glucose level in frogs kept at
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Acknowledgments br INTRODUCTION AND OBJECTIVES br METHODS br
2021-12-23
Acknowledgments INTRODUCTION AND OBJECTIVES METHODS RESULTS CONCLUSIONS Introduction Class 3 alcohol dehydrogenase (EC 1.1.1.1), also known as ADH5 chi polypeptide in humans, was first identified by Koivusalo et al. [1] as a NAD+-dependent hydroxymethylglutathione (HMGSH) oxidase. By
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br Conclusions br Competing interests br Introduction
2021-12-23
Conclusions Competing interests Introduction Ethanol exposure has been linked to changes in the pattern of histone acetylation and deacetylation through histone acetyltransferases (HATs) and histone deacetylases (HDACs) in the gap-26 and in peripheral tissues, leading to ethanol dependence-
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Since KYNA concentrations are increased by
2021-12-23
Since KYNA concentrations are increased by aerobic exercise training, we have investigated if it plays a role in peripheral tissue metabolism. Here we show that KYNA regulates adipose tissue energy homeostasis through activation of Gpr35. Activation of this network stimulates the expression of lipid
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