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In summary the SAR of
2022-02-26

In summary, the SAR of a series of phenylpropanoic acid-free fatty niclosamide synthesis 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
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The central event eliciting insulin secretion is the product
2022-02-26

The central event eliciting insulin secretion is the production of ATP which leads to the inhibition of ATP-sensitive inwardly-rectifying K+ATP channels, a consecutive depolarization of the plasma membrane with opening of voltage-dependent Ca2+ channels and Ca2+ influx into the beta-cell. However, i
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br Material and methods br Acknowledgements and funding The
2022-02-26

Material and methods Acknowledgements and funding The authors thank Katharina Elsässer for technical support and Emma Esser for careful editing of the manuscript. We also thank Marcus Conrad for providing Liproxstatin-1 and advisory comments and discussion on the manuscript. This work was part
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As recently reviewed a picture is emerging where
2022-02-26

As recently reviewed, a picture is emerging where metabolites through GPCR sensors act as important autocrine and paracrine regulators of basic metabolic mechanisms (Husted et al., 2017). The concept of 20-HETE acting through FFAR1 as an autocrine amplifier of GDIS on β Kif15-IN-1 together with, for
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Syt itself does not catalyze lipid mixing
2022-02-26

Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisel
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br Conflict of interest statement br References and recommen
2022-02-26

Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We thank Urann Chan for assistance with the figures. This work was supported in part by National Institutes of
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br Conclusions Histone acetylation deacetylation is
2022-02-26

Conclusions Histone acetylation/deacetylation is a major epigenetic mechanism implicated in the regulation of transcription and various biological processes such as development and gametogenesis from plants to vertebrates. However, despite being well characterized in zebrafish, acetyltransferase
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This crosstalk may be responsible
2022-02-26

This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on NHS-SS-Biotin pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-dose ra
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Fludara Newly identified evidence has put immune checkpoint
2022-02-26

Newly identified evidence has put immune checkpoint inhibitors into the spotlight. However, even though they have been reported to achieve optimistic outcomes [67], there is still a provocative question about their limitations [68]. The solid evidence above has provided us with translational values
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In autoimmune diseases lymphocytes penetrate into the inflam
2022-02-26

In autoimmune diseases, lymphocytes penetrate into the inflammatory lesions of tissues, where it is prominently hypoxic or even anoxic, and utilize glycolysis for an energy supply after activation or under hypoxia (Sitkovsky and Lukashev, 2005; Palazon et al., 2014), which is modulated by the oxygen
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br Materials and methods br Results br Discussion Dex
2022-02-25

Materials and methods Results Discussion Dex has been shown to induce apoptosis in osteoblastic cell lines (MC3T3-E1, UAMS-32 cell) [24], [25]. Consistent with previous reports, we find high-dose Dex (1 or 5 μM) can induce apoptosis of MC3T3-E1 ursolic acid within 24 h as evidenced by Anne
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Introduction Heme is an important small molecule and an esse
2022-02-25

Introduction Heme is an important small molecule and an essential cofactor for a variety of enzymes (George, 1948; Morrison and Stotz, 1954; Maehly, 1952; Igo et al., 1961). During cellular respiration, heme populates cytochromes and serves as an electron acceptor in the electron transport chain (M
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The dramatically reduced expression of CFTR
2022-02-25

The dramatically reduced expression of CFTR in human colorectal cancer tissues identified herein is consistent with our previous findings using human breast cancer tissues, prostate cancer tissues, and colon cancer tissues, and suggests that the loss of CFTR is likely a general phenomenon in epithel
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HCV is a highly diverse virus with seven known genotypes
2022-02-25

HCV is a highly diverse virus with seven known genotypes (GT1–7) and multiple subtypes (Gower et al., 2014, Messina et al., 2015, Smith et al., 2014). Patients infected with HCV develop a heterogeneous population of viral species known as quasispecies due to low fidelity of the RNA-dependent RNA pol
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br Conclusions br Introduction Astrocytes contribute to
2022-02-25

Conclusions Introduction Astrocytes contribute to physiological EPZ031686 function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with energy subs
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