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This excellent tolerability is especially interesting
2022-03-26
This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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Recently we indicated that cell motility was regulated
2022-03-26
Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 orotic acid treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) which is a potent
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Active compounds and were further tested and
2022-03-26
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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However at variance with the well studied
2022-03-26
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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This study was supported by the Finance Department
2022-03-26
This study was supported by the Finance Department Foundation of Jilin Province (3D5178963428). Introduction Breast cancer is one of the leading cause of death in women worldwide [1,2]. Due to recent advances of combined therapies, survival rate of breast has improved significantly. However, bre
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Spindle positioning is governed by the
2022-03-26
Spindle positioning is governed by the actin cytoskeleton. After a transient metaphase arrest, cells lacking haspin exhibit a misdistribution of actin, which accumulates within the bud. Actin dynamics is modulated by an intricate network including septins, the polarisome complex, and formins. We sho
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Introduction Inorganic arsenic InAs species such as arsenite
2022-03-26
Introduction Inorganic arsenic (InAs) species such as arsenite (AsIII) and arsenate (AsV) are present in groundwater. Arsenic contaminated drinking water is a global public health issue because of its natural prevalence and toxicity. Long exposure to arsenic results in chronic effect in humans, inc
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Despite the similarities there are
2022-03-26
Despite the similarities, there are some differences between the augmentation by hypoxia and that by thymoquinone. While in porcine coronary arteries they both depend on calcium sensitization mediated by ROCK12, 32, 33, L-type calcium channels are involved only in thymoquinone-induced augmentation.
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br Cellular directionality To obtain a comprehensive underst
2022-03-26
Cellular directionality To obtain a comprehensive understanding of cell migration, it is essential to understand how cues from the cell’s external environment are relayed to the Cilostazol cytoskeleton, so the cell can migrate towards the cue; a process herein referred to as cellular directional
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In summary we have successfully identified a series
2022-03-25
In summary, we have successfully identified a series of potent and selective GSNOR inhibitors having imidazole and tetrazole functional groups in both end of the core structure and many compounds have been identified with IC: Introduction Peppers (Capsicum annuum L.), tomatoes and potatoes, belon
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Armed with this knowledge we looked at ways to reduce
2022-03-25
Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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Over expression of Glo can suppress inflammatory responses M
2022-03-25
Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial omadacycline [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen exp
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urat1 inhibitor In summary activated A AR
2022-03-25
In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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br GluR A knockout mice Genetically modified adult
2022-03-25
GluR-A knockout mice Genetically modified, adult mice lacking the GluR-A AMPA receptor subunit exhibit fast synaptic transmission in the hippocampus, mediated by the receptors formed from the remaining AMPA receptor subunits GluR-B and GluR-C (Sommer et al., 1991), but are deficient in a rapidly
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br Summary br Acknowledgement br GR A Nuclear Receptor
2022-03-25
Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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