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A number of in vivo studies
2022-06-28

A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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Continuing studies of endocannabinoid ligands at GPR
2022-06-28

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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The pharmacokinetics of was obtained in
2022-06-28

The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indicat
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Hesperidin is an abundant and inexpensive plant flavonoid la
2022-06-28

Hesperidin is an abundant and inexpensive plant flavonoid, largely derived from citrus species including sweet orange and lemon. Hesperetin (Hst) is the aglycone of hesperidin. Hesperidin and hesperetin have been reported to show a battery of pharmacological properties, including anti-hyperlipidemic
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VU 591 hydrochloride mg br Materials and methods br
2022-06-28

Materials and methods Results Discussion Since 1990s, solving structures for most DNA glycosylases by X-ray crystallography significantly advanced mechanistic understanding of the catalytic activity and substrate specificity of this important class of DNA repair enzymes. However, static str
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br Methods and materials br Results and discussion br Conclu
2022-06-28

Methods and materials Results and discussion Conclusions This is the first study that attempted to isolate, purify and identify the characteristics of ataluren from ginseng. In vitro studies have demonstrated that PGL-1 efficiently suppressed SH-SY5Y cell apoptosis induced by Aβ25–35, poss
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Tetrazole is one of the most commonly
2022-06-28

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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Ghrelin contains an n octanoylation at its Ser residue Kojim
2022-06-27

Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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In order to test the influence of the initial
2022-06-27

In order to test the influence of the initial depolarization, experiments were performed, where the degree of chloride substitution was varied, either by adding n-Ringer to dichloroacetate mg incubated in a sucrose Ringer or by suspending the cells directly in Ringers identical to the final composi
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br Materials and methods br
2022-06-27

Materials and methods Results and discussion Conclusions Acknowledgements This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2013 unit and COMPETE 2020 (POCI-01-0145-FEDER-006684), and also by t
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br Introduction Thrombosis is one of the leading
2022-06-27

Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable p38 pathway and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (1–2
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As for all DOACs measurement of DiXaIs
2022-06-27

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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br STAR Methods br Acknowledgments
2022-06-27

STAR★Methods Acknowledgments We thank the Shanghai Synchrotron Radiation Facility (SSRF) BL18U for help with X-ray data collection. We thank Dr. Thomas F.J. Martin for providing the pcDNA3.1-CAPS-1 plasmid and Dr. Xiaofei Yang for providing the pFHUUIG_shortU6 (l309) plasmid. We thank Dr. Shun
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To understand the structural basis for
2022-06-27

To understand the structural basis for the mode of action of indole-based compounds the crystal structures of bound to both the wild type and A128T IN CCDs have been solved. The X-ray crystallography studies have revealed that binds at the IN dimer interface in the principal LEDGF/p75 binding pock
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The VirScan assay has several advantages over alternative mu
2022-06-27

The VirScan assay has several advantages over alternative multiplex serological assays for peptide discovery. These advantages include quantitative assessment of antibody binding to peptides that span all open reading frames in the HIV genome, including both structural and regulatory proteins; repre
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