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Ryoichi et al modified potent
2024-12-18

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Fencilli et al reported derivatives of PHA which demonstrate
2024-12-18

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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br Experimental section br Competing interests br Author s
2024-12-18

Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig
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Earlier studies showed that exposure of cells to IR
2024-12-18

Earlier studies showed that exposure of cells to IR caused ATM-dependent phosphorylation of 53BP1, as judged by electrophoretic mobility shift [24], [25], [26]. To date, the only known in vivo 53BP1 phosphorylation site(s) are Ser25 and possibly Ser29 [27]. In the course of our studies, we noticed t
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Telomerase action at the telomere is highly regulated it pre
2024-12-18

Telomerase action at the telomere is highly regulated; it preferentially elongates the shortest telomeres, and recruitment of the enzyme complex to the telomere occurs in mid-S phase of the cell cycle (Bianchi and Shore, 2007, Britt-Compton et al., 2009, Teixeira et al., 2004, Hemann et al., 2001, T
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br Conclusions and future direction ER PgR
2024-12-18

Conclusions and future direction ER(−)/PgR(+) breast cancers have a distinct clinical course, response to treatment, and molecular features when compared to other breast cancer types, however some of them are actually technical artifacts or consequences of too high definitions of positivity. Acco
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br Extracellular domain architecture The extracellular regio
2024-12-18

Extracellular domain architecture The extracellular region of GABAB receptor exists in a heterodimeric configuration regardless of interactions within the rest of the protein (Geng et al., 2012, Liu et al., 2004, Nomura et al., 2008). The extracellular domains of the GABAB1 and GABAB2 subunits ar
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Our surprising results show that AAD treated tumors
2024-12-17

Our surprising results show that AAD-treated tumors adjacent to adipose tissues and in steatotic liver continue to grow in the presence of a minimal number of microvessels. In non-adipose tumor models, the similar degree of vascular suppression is translated into marked suppression of tumor growth.
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However a high triglyceride level was
2024-12-17

However, a high triglyceride level was associated with dementia in a study with subjects aged ≥65 years (Raffaitin et al., 2009). In another study, the serum triglyceride levels of three different transgenic mouse strains mimicking AD were also evaluated within the progression of the pathology. In o
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br Materials and methods br Results br Discussion Knowledge
2024-12-17

Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Introduction A defining feature of cancer
2024-12-17

Introduction A defining feature of cancer cells is disruption of the normal controls of the cell cycle; a tumor suppressor or inhibitor may act by restricting progression of the cell cycle. P27 (also known as cyclin-dependent kinase inhibitor 1B, P27, or Kip1) is a putative cell-cycle inhibitor pro
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br Liver specific AHR deficiency and energy balance In
2024-12-17

Liver-specific AHR deficiency and energy balance In contrast to the amelioration of hepatic steatosis by global AHR deficiency, targeted knockout of Ahr in hepatocytes exacerbated it in B6 mice fed on a high-fat diet, without interfering with body weight gain [21]. This appeared to result from au
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br Conclusion br Conflict of
2024-12-17

Conclusion Conflict of interest Acknowledgments We thank Nancy Kerkvliet for helpful advice. The research in the lab of CE and THS is supported by the Deutsche Forschungsgemeinschaft (grants ES103/7-1 and 9-1, HA7346/2-1). We apologize to all authors whose work could not be cited due to lim
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br Experimental Procedures br Acknowledgments br Introductio
2024-12-17

Experimental Procedures Acknowledgments Introduction Synapses are fundamental units for efficient communication between neurons and their target cells. Despite significant progress in understanding the structure of matured synapses, less is known about the mechanisms by which neurotransmitt
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Search sphere This sphere includes the acetylcholine binding
2024-12-17

Search sphere 1: This sphere includes the Guanethidine Sulfate binding site between the α–γ subunits. The center point of the search area was located at x=35.26, y=77.67, z=137.74 and the initial search radius was set to 27Å which assures that the corresponding area outside the channel pore of the t
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