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br Experimental Procedures Information on the materials
2021-12-09

Experimental Procedures Information on the materials used in this study and the details of how the in vivo and in vitro assays were performed are provided in Supplemental Information. Acknowledgments This research was supported by the National Research Foundation of Korea (NRF) grant funded b
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The overall very satisfactory potency profile of compounds a
2021-12-09

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Pentostatin core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly s
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br General features of FGFRs and
2021-12-09

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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Introduction High mobility group box HMGB is a nuclear
2021-12-09

Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various
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Several classes of small molecule
2021-12-09

Several Gedunin synthesis of small-molecule inhibitors of FBPase have been reported. These inhibitors can be structurally classified into two groups; non-phosphorus-based inhibitors and phosphorus-based inhibitors. In the former group, several chemotypes including anilinoquinazoline, indole dicarbo
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To explain the corporate debt maturity following
2021-12-09

To explain the corporate debt maturity, following Brockman et al. (2010), the time-varying control variables we include are: firm size (LSIZE), the square of firm size (LSIZE2), leverage (LEVERAGE), asset maturity (ASSET_MAT), managerial ownership (OWN), market-to-book ratio (MB), term structure of
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As for all DOACs measurement of DiXaIs activity
2021-12-09

As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe
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Mammals adapt to prolonged periods of food
2021-12-09

Mammals adapt to prolonged periods of food scarcity by releasing FFAs from adipose tissue and transforming them into energy-rich ketone bodies that are used as fuel by brain, muscle, and other organs (Kersten, 2014, Grabacka et al., 2016). Ketogenesis occurs primarily in hepatocytes, but its rate is
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We observed that the Toc G domain recognizes the N
2021-12-08

We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate
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br Conflicts of interest br
2021-12-08

Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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CL 316243 disodium salt MAPK are involved in a
2021-12-08

MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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br The small conductance Ca activated K
2021-12-08

The small conductance Ca-activated K+ (SKCa; SK, SKCa, KCa2) channels are recognized as a subfamily of KCa channels (Bond, Maylie, & Adelman, 1999). The SKCa channel is encoded by three distinct genes, KCNN1, KCNN2, and KCNN3 with different sensitivities toward apamin. Different with BKCa channels
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br Some general considerations on anterior pituitary
2021-12-08

Some general considerations on anterior pituitary cell type, models, sex and drugs Historically, real-time analysis of native endocrine anterior pituitary cell excitability has been somewhat limited and thus much of the pioneering work on anterior pituitary cell excitability and stimulus-secretio
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br Although D reconstruction of
2021-12-08

Although 3D reconstruction of an invertebrate gap junction channel from native tissue of crayfish was reported in 1991, the negative-staining EM imaging was limited to low-resolution structural analysis [39]. The oligomeric number of innexin channels was believed to be the same as that in connexin
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Interestingly we have shown that OA
2021-12-08

Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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