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The identification of novel kinase inhibitor scaffolds is hi
2024-12-27
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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Hypoxia induced replication arrest has been demonstrated in
2024-12-27
Hypoxia-induced replication arrest has been demonstrated in a variety of organisms in addition to mammals; including Zebrafish , , and (brine shrimp) which have been shown to survive for 4 years and longer in anoxic conditions . Despite this breadth of study, little is known about the mechanism of
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Obesity is associated with chronic low grade
2024-12-27
Obesity is associated with chronic low-grade mineralocorticoid receptor antagonists resulting from increased M1 macrophage infiltration into adipose tissue, which can subsequently lead to the development of insulin resistance. Previously, we reported that LFE and FSB both reduced body weight gain i
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br Author Contributions br Acknowledgments
2024-12-27
Author Contributions Acknowledgments Introduction Cerebral ischemia-reperfusion (I/R) injury is a pathological phenomenon that occurs after restoration of blood supply to Intracellular ROS detection tissues subsequent to ischemia or hypoxia (Carden and Granger, 2000). It typically occurs a
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The expanding catalog of glutamate
2024-12-27
The expanding catalog of glutamate receptor auxiliary subunits and associated transmembrane proteins underscores the importance and complexity of the receptor complexes. Whereas the interactions described here specifically control AMPARs, distinct auxiliary subunits, Neto-1/2, modulate neuronal kain
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Imatinib was first approved for the treatment
2024-12-27
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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br Conclusion br Conflict of interest
2024-12-27
Conclusion Conflict of interest Introduction Oral cancer may originate from lips, lower and upper alveolar ridges, hard palate, sublingual region, buccal mucosa, anterior two-thirds of the tongue as well as retromolar trigone and floor of the mouth (World Health Organization, 2013). As the
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br Conclusion br Conflict of interest
2024-12-27
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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While HTPCs are not immune cells they produce IL
2024-12-27
While HTPCs are not immune cells, they produce IL-6, MCP-1 and other immunologically relevant factors (Mayer et al., 2016). Our results demonstrated that epinephrine and phenylephrine increased the mRNA expression levels of COX-2, IL-6 and MCP-1 in HTPCs without affecting the mRNA expression level o
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Derivatives of M that possess either an
2024-12-26
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these NS-398 to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrated t
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myo d chiro inositol In the late s Solvay Pharmaceuticals di
2024-12-26
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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br Results br Discussion Utilizing a
2024-12-26
Results Discussion Utilizing a proteomic approach, we identified HSP90β as a protein that becomes associated with surface AChR in agrin-stimulated muscle cells. We demonstrate that HSP90β does not interact with the AChR directly; instead, via direct interaction with rapsyn, HSP90β becomes asso
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Finally Urban Ciecko et al asked whether this
2024-12-26
Finally, Urban-Ciecko et al. (2018) asked whether this enhancement is specific to the pyramidal to SST neuron synapses or more generally observed in other synapses of the cortical microcircuit. Synapses between pyramidal cells showed no sign of potentiation after either bath application of the choli
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The inhibition of the exacerbated inflammatory
2024-12-26
The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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The present study showed for the first time that
2024-12-26
The present study showed, for the first time, that hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, and isocorynoxeine in yokukansan can inhibit the 5-HT3 receptor current. These data indicate that part of the effect of yokukansan against the behavioral and psychological symp
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