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br Conclusions There is significant interest
2020-12-07
Conclusions There is significant interest in understanding the contribution of biological mechanisms to the non-linear/bilinear dose–response curves for DNA-reactive agents. Model monofunctional alkylating agents have datasets amenable to PoD determination for genotoxic effects in both in vitro a
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br DGKs inhibition and signaling
2020-12-07
DGKs inhibition and signaling Local DAG levels are strictly controlled by a balance between synthesis and degradation rates. Both receptor controlled PLC-mediated production and DGK-mediated degradation are classically implicated in the control of “signaling” DAG. However, this dogma is starting
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ApicomplexansApicomplexans are unicellular and spore
2020-12-07
ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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Although the crystal structures of Atg C and Atg
2020-12-07
Although the crystal structures of Atg4C and Atg4D are not available, their three dimensional structures can be acquired by homology modeling, using the structure of Atg4B as a template (Zhang, Li, Ouyang, Liu, & Cheng, 2016). In that model, the catalytic triad is conserved (Cys110/Asp345/His347 for
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Given the importance of cysteine cathepsin inhibitors as put
2020-12-07
Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2020-12-04
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase bosentan receptor [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour
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dilution equation The following is the supplementary data
2020-12-04
The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter
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Sensory gating describes a filter mechanism protecting the c
2020-12-04
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits SU11274 to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). Auditory ga
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Due to its several industrial applications the
2020-12-04
Due to its several industrial applications, the recombinant production of collagen and all its derivatives as gelatins has been pursued for many years in different biological systems as mammalian glucokinase inhibitor (Toman et al., 1999), tobacco plants (Ruggiero et al., 2000), silkworms (Tomita et
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During ischemia the impact of CK on mitochondria varies in
2020-12-04
During ischemia, the impact of CK2 on mitochondria varies in different organs/tissues. For example, CK2α upregulation during ischemia leads to disrupted mitochondrial homeostasis and mediates cardiomyocyte ischemic injury [31]. Specifically, ischemia/reperfusion (I/R) progressively increases CK2α to
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br Acknowledgements This work was
2020-12-04
Acknowledgements This work was supported by a grant from the Deutsche Forschungsgemeinschaft to Uwe Knippschild and Martin Wabitsch (SFB 1149/B4). P. Fischer-Posovszky is funded by a Margarete von Wrangell scholarship financed by the Ministerium für Wissenschaft, Forschung und Kunst Baden-Württem
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br Introduction Ewing s sarcoma
2020-12-04
Introduction Ewing’s sarcoma (ES) is a mesenchymal tumor characterized by small, round, blue cells, and is poorly differentiated and highly malignant [1]. While ES typically arises in bone and soft tissue, rare primary extraosseous manifestations of ES have been reported throughout the body [2].
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Importantly a crucial role of transcription
2020-12-04
Importantly, a crucial role of transcription factor SP1 in mediating the anti-lung cancer effect of XJD was found in this study. Our results suggested that the inhibition of SP1 was required to mediate the inhibitory effect of XJD on the growth of NSCLC cells. Nuclear transcription factors SP1 is as
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Compared to ET all agonists tested showed
2020-12-04
Compared to ET-1, all agonists tested showed a 2–4 fold bias for the G protein constrictor assay compared to the β-arrestin assay (Table 1). This preliminary analysis indicated that at least modest pathway bias for endogenous ET peptides is possible, however the physiological significance of this, i
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PKA signalling in the nucleus
2020-12-04
PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the AL 8810 to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been identified in the nucleus and funct
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