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We have previously designed an azobenzene based molecule Raz
2021-11-25
We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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In terms of cytotoxicity studies
2021-11-25
In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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EZH can also interact with Ten Eleven Translocation gene fam
2021-11-25
EZH2 can also interact with Ten-Eleven Translocation gene family members (TET1, TET2, and TET3), which convert 5-methylcytosine (5 mC) to 5-hydroxymethylcytosine (5hmC), to cause changes in patterns of histone methylation and DNA methylation [52]. Huang et al. found that the expression levels of all
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The third group also included samples belonging to
2021-11-25
The third group also included samples belonging to subjects with undetectable viraemia, for which the negative or persistence of the indeterminate WB result in subsequent samples indicated a non-HIV infection. In this subgroup, the VITROS HIV Combo test (as well as the other two tests) was negative
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Based on the aforementioned findings variations of the imida
2021-11-25
Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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There were limitations to this study
2021-11-25
There were limitations to this study. Specifically, although rigorously examined for accuracy, the NCDB and SEER databases still suffer from issues with data entry and completeness of the treatment record. Of note, although the data were collected on a modern cohort of patients treated from 2010 to
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Compound containing dimethylglutarimide P cap P
2021-11-25
Compound containing, dimethylglutarimide P-cap, P propyl group, α-methylbenzyl urea resulted in inhibitor with much improved binding (=0.064μM) and EC=0.3μM. This was an aza-peptide analog with an EC comparable to our first generation clinical candidate . Analog was evaluated for its selectivity
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CGP 41251 It was revealed that various
2021-11-25
It was revealed that various injured or infected organs of Hippeastrum produce a mixture of an orange-colored chalcone and flavans which can be oxidized to red-colored dimer (Wilmowicz et al., 2014, Wink and Lehmann, 1996), preventing the penetration of injured tissues by Phoma narcissi, Botrytis ci
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Interestingly systemic circulating levels of
2021-11-25
Interestingly, systemic circulating levels of NOx were not dramatically increased by treatment with isosorbide mononitrate or sodium nitrite at a dose which exerted beneficial effects on the progression of PH. In line with our results, Mathew et al. [13] demonstrated that the long-acting NO donor mo
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The following are the supplementary data related to this
2021-11-24
The following are the supplementary data related to this article. Author contribution Conflict of interest Introduction Thrombosis (arterial and venous) is a major cause of vascular obstructive diseases including myocardial infarction, cerebral infarction and pulmonary embolism. Glycoprote
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br Brief overview of the glutamate system and rationale for
2021-11-24
Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric CKI 7 dihydrochloride (GABA), the primary inhibitory neurotransmitter.
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After brain injury adenosine levels rapidly increase in
2021-11-24
After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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To study the effects of GPR at the whole
2021-11-24
To study the effects of GPR40 at the whole-animal level, GPR40 mice have been generated in two different genetic backgrounds [18], [19]. GPR40 mice from both backgrounds were apparently healthy with no overt signs of metabolic or other abnormalities. As expected, pancreatic islets taken from GPR40
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br The small conductance Ca activated K SKCa
2021-11-24
The small conductance Ca-activated K+ (SKCa; SK, SKCa, KCa2) channels are recognized as a subfamily of KCa channels (Bond, Maylie, & Adelman, 1999). The SKCa channel is encoded by three distinct genes, KCNN1, KCNN2, and KCNN3 with different sensitivities toward apamin. Different with BKCa channels
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During the course of the development of aminothiazole
2021-11-24
During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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