• Glimepiride Here we report discovery of

  2024-10-29

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Glimepiride bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To

• We used the lead compound

  2024-10-29

  

  We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.

• br Experimental Procedures br Acknowledgments This

  2024-10-29

  

  Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI)R00 HG006922 and NIH/NHGRIR01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research repor

• br Materials and methods br Results In

  2024-10-29

  

  Materials and methods Results In order to evaluate changes in the amount of PKC-θ expressed by MEL cells at different stages of the cell cycle, we measured the level of the kinase in cells collected from cultures containing 90% of cells in the interphase or 80% cells synchronized at the metaph

• Since artemisinin shows low solubility and poor oral bioavai

  2024-10-29

  

  Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-

• br Summary br Introduction With readily synthetic methods

  2024-10-29

  

  Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually, o

• br AR signaling and urothelial cancer progression As shown

  2024-10-29

  

  AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et 

• br AKT signaling is essential during early dorsal patterning

  2024-10-28

  

  AKT signaling is essential during early dorsal patterning, neural crest induction and maturation AKT signaling modulates EMT and migration of the neural crest cells The defining feature of NC cells is their delamination from the dorsal neural epithelium. At the end of neurulation, mature premi

• ON123300 Mast cells Mast cells are immune

  2024-10-28

  

  Mast cells. Mast ON123300 are immune cells of the myeloid lineage and are ubiquitously present in connective tissues [75]. These cells are involved in the modulation of a number of physiological functions, such as vasodilation, angiogenesis, bacterial, and parasite elimination [75]. Moreover, mast

• Introduction Microdialysis is an in vivo technique

  2024-10-28

  

  Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the

• The major strength of this study is the

  2024-10-28

  

  The major strength of this study is the large sample size which increases the statistical power to detect the likely subtle differences in peripheral methylation observed in psychiatric disorders (Olsson et al., 2010). Larger studies help provide more robust estimates of true associations, as small

• Introduction Dementia is a common disease in

  2024-10-28

  

  Introduction Dementia is a common disease in the elderly, and a significant source of disability, healthcare spending, and long-term care admissions. There is evidence to suggest that testosterone plays a role in cognitive functioning, and lower serum levels correlate with higher amyloid deposits (

• PF also a dual Aurora A and Aurora B

  2024-10-28

  

  PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly WY-14643 synthesis for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD

• Two critical determinants of receptor trafficking are found

  2024-10-28

  

  Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al

• br Author contributions br Acknowledgments TJC KW and VG

  2024-10-28

  

  Author contributions Acknowledgments TJC, KW, and VG are supported by awards made to MJN: a Consolidator Grant from the European Research Council under Grant no. 311336; a University Research Fellowship from the Royal Society, and a Career Development Award from the Human Frontiers Science Pro

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