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A general synthetic pathway to these tricyclic structures is
2021-10-23

A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy
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Recently a G protein coupled receptor
2021-10-23

Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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It may seem counterintuitive that a lymphocyte which is
2021-10-23

It may seem counterintuitive that a lymphocyte which is unable to proliferate could have neoplastic potential since the very definition of neoplasia is one of autonomous clonal expansion of a cell. The lack of co-stimulatory molecules CD27 and CD28 can potentially be overcome by activating NK cell r
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br Acknowledgments This work was supported by the
2021-10-23

Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE010200
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Bergmann glia cells BGCs are the most abundant
2021-10-23

Bergmann glia 5ht receptors (BGCs) are the most abundant glia cells in the cerebellum, comprising more than 90% of the cerebellar glia. These cells span the entire cerebellar molecular layer and encapsulate neuronal somata, dendrites and axons. BGC are involved in neurotransmitter uptake, K+ homeos
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An increased sympathetic tone and the hormone glucagon are
2021-10-23

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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br General features of FGFRs and inhibitors br Conclusion Gi
2021-10-22

General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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br Clinical assessment of iron chelation br
2021-10-22

Clinical assessment of iron chelation Towards the new concept of conservative iron chelation: iron scavenging and redeployment For any chelator to be of clinical value in disorders of regional siderosis they ought to be endowed with a requisite accessibility to the relevant sites and different
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Several recent studies have linked clock
2021-10-22

Several recent studies have linked clock function with the cell cycle and reported that clock components, such as PER1, PER2, BMAL1, and CRY1/2 decrease cell proliferation or improve the action of anti-cancer drugs in different cancer cell lines. Moreover, certain types of human cancer show an alter
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br Conclusion br Acknowledgments This research was funded by
2021-10-22

Conclusion Acknowledgments This research was funded by Tianjin Health Institution Key Projects, grant number 15KG148” and “Tianjin Medical University General Hospital Youth Incubation Fund, grant number ZYYFY2017029”. I would like to express my heartfelt gratitude to Professor Hongtao Zhang fo
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The absence of direct oxidation
2021-10-22

The absence of direct oxidation of Fe2+ by L1 in experiments in solution would be consistent with the recognized low O2 affinity of sGC. It is known that, in palmitic acid receptor with other hemoproteins, such as globins and heme-containing oxygenases with a Fe2+-proximal histidine linkage, sGC pre
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br Rho protein networks in malignancy It has
2021-10-22

Rho protein networks in malignancy It has long been recognized that Rho activity and expression are frequently elevated in tumors (Fritz et al., 1999, Orgaz et al., 2014). In this chapter we will introduce the most prominent Rho proteins, their regulators and effectors and provide an overview of
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br Funding This work was partially supported by
2021-10-22

Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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All HFD fed groups in our
2021-10-22

All HFD fed groups in our study, having significantly higher levels of EE (heat production) is consistent with previous studies [91], where a significant increase in EE was observed within just one week of HFD feeding [81]. It is hypothesized that this phenomenon is due to the increased body mass an
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br Material and methods br Results Consistent with
2021-10-22

Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing Ertapenem sodium salt synthesis in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involv
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