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Here we report discovery of highly
2023-03-22
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of 3902 australia 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.
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L-Arabinose Several mechanisms have been suggested to accoun
2023-03-22
Several mechanisms have been suggested to account for the causal association of ICAM-1 induction and leukocyte adhesion with DR, including oxidative stress [16], NF-κB [17], PKC [18], and bioactive lipids [19]. Our previous studies highlighted the role of bioactive lipid metabolites derived from 12/
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Protein phosphorylation is an important posttranslational me
2023-03-22
Protein phosphorylation is an important posttranslational mechanism for the regulation of distribution, trafficking, and function of modified proteins (Wang et al., 2014). GluA1 phosphorylation at S845 also has functional consequences (Lu and Roche, 2012). For instance, S845 phosphorylation drove tr
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Finally intracrine androgen synthesis metabolism can
2023-03-20
Finally, intracrine androgen synthesis/metabolism can be activated thus allowing Tunicamycin to bypass the low levels of androgens in the circulation by producing androgens themselves (Cai and Balk, 2011, Rahman et al., 2004). Moreover, changes in AR co-regulators like the overexpression of steroid
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Cancers that responded to immune checkpoint
2023-03-20
Cancers that responded to immune checkpoint inhibitors were shown to present a type I interferon (IFN) signature in the TME 33, 34. Type I IFNs positively regulate the expression of tumor antigens and their crosspresentation by DCs to tumoricidal CTLs. Furthermore, CD8+ T cell develops full effector
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br Conclusion br Conflict of Interest br
2023-03-20
Conclusion Conflict of Interest Author Contributions Acknowledgements This work was supported by a research grant (SR/50/AS-14/2012) from the Department of Science and Technology, New Delhi, India to CMC and CSIR Senior Research Fellowship (09/013(0339)/2010-EMR-I) to SB. Introduction
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The cellular mechanism underlying the CGS
2023-03-20
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Fisetin Another open question is whether GABA and
2023-03-17
Another open question is whether GABA and ACh are released from the same synaptic vesicles, or even the same presynaptic terminals. Multi-transmitter neurons may either function through co-release, in which multiple neurotransmitters are packaged into the same presynaptic terminal and are therefore
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The present study showed for the first
2023-03-17
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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br Acknowledgements This work was supported by the FedEx Ins
2023-03-17
Acknowledgements This work was supported by the FedEx Institute of Technology at The University of Memphis (to DLB and ALP), NSF REU CHE 1156738 (to ALP in support of RSS), and NIHCA921060 (to GT). This material is based upon work supported by the National Science Foundation under Grant No. CHE-1
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br Materials and methods br Results To explore
2023-03-17
Materials and methods Results To explore the potential role of autophagy in drug resistance, we firstly performed immunohistochemistry to compare the Stattic of p62 in paired primary, metastatic, and recurrent tumor tissues from 26 ovarian cancer patients. The expression of p62 was revealed t
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calcium calmodulin dependent protein kinase TUNEL assay Apop
2023-03-17
TUNEL assay. Apoptotic DNA fragmentation in calcium calmodulin dependent protein kinase was measured using a commercially available TUNEL assay kit (Thermo Fisher). Frozen cells were fixed with 10% paraformaldehyde/PBS. Apoptosis was determined by staining the 3′-OH ends of fragmented DNA with bioti
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The results of our in vivo experiments provide promising
2023-03-17
The results of our in vivo experiments provide promising evidence that the apelin/APLNR axis is implicated in CCA growth and that targeting this axis with a receptor specific antagonist may help develop effective, tumor directed therapies. Not only do we show decreased proliferation and angiogenesis
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br Nanoparticle Conjugated Topoisomerase Inhibitors The safe
2023-03-17
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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br Funding br Introduction Plants absorb both inorganic
2023-03-17
Funding Introduction Plants absorb both inorganic nitrogen (ammonium and nitrate) and organic nitrogen (amino acids and peptides) from the soil [1]. The first organic nitrogenous molecule produced from inorganic nitrogen is Gln, whose terminal amino group is successively transferred to make Gl
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