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Determination of enzyme activity differs from other analytic
2021-11-26
Determination of enzyme activity differs from other analytical procedures. In this cgrp antagonist case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic
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DNAzymes a series of nucleotide sequences with specific
2021-11-26
DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN
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Receptor interactions and binding mode
2021-11-26
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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br Ferroptosis modulators With the recognition that the smal
2021-11-26
Ferroptosis modulators With the recognition that the small molecule erastin targets system xc- and thereby specifically triggers this form of death and that ferrostatin-1 prevents erastin-induced ferroptosis [2], it has become evident that ferroptosis is a druggable pathway with a number of tract
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Histone demethylases are involved in the transcriptional out
2021-11-26
Histone demethylases are involved in the transcriptional output of the AR and hypoxia signaling pathways, and thus contribute to prostate cancer development [12]. For example, the histone demethylase KDM3A serves as a transcriptional coactivator of HIF1α and AR in regulation of their target genes [1
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Furthermore Rosethorne and Charlton Panula et al Reher et
2021-11-26
Furthermore, Rosethorne and Charlton (Panula et al., 2015, Reher et al., 2012, Rosethorne and Charlton, 2011) expressed the human H4R in an osteosarcoma cell line and found that with respect to [35S]GTPγS binding, JNJ-7777120 acted as a neutral antagonist or very weak inverse agonist, a finding whic
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It was speculated that could affect
2021-11-26
It was speculated that could affect the protein translation or processing in the HCV replication cycle. The viral protein processing was thus investigated, to establish whether the HCV inhibition was determining an increased amount of unprocessed polyprotein, due to a block in the processing, or a
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The biological function of NPRA is
2021-11-26
The biological function of NPRA is demonstrated primarily through the ANP/BNP-dependent GC catalytic activity of the receptor and the production of cGMP, which is regulated by several factors, including hormones, growth factors, physiological milieu, and the ligand itself [26,34,[36], [37], [38], [3
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br Conclusions br Acknowledgement br Introduction The macrop
2021-11-26
Conclusions Acknowledgement Introduction The macrophage is an important cell species that plays key roles in innate immune responses and inflammatory reactions through phagocytosis of foreign bodies and secretion of inflammatory mediators such as interleukin (IL)-1, tumor necrosis factor (T
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br Introduction Nicotinic acid has been used clinically
2021-11-26
Introduction Nicotinic SynaptoRedTM C2 has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HDL-C) [2]. Nicot
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Antibiotic treatment suggests that cancer promoting
2021-11-26
Antibiotic treatment suggests that cancer-promoting bacteria arise from the Oxamic acid of Grp109a mice. How does the lack of Gpr109a signaling lead to expansion of potentially cancer-promoting bacteria? Is this phenomenon related to improper development of intestinal Treg cells? Biome with cancer-
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One effective approach to fine tuning the lipophilicity
2021-11-25
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic GSK 2830371 scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as Am
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A breakthrough in the understanding of the
2021-11-25
A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty GSK1904529A metabolizing enzyme [92], in the execution of GPX4-knockout
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Biapenem br Introduction Fructose bisphosphatase FBPase
2021-11-25
Introduction Fructose 1,6-bisphosphatase (FBPase; EC 3.1.3.11) catalyses the irreversible reaction of hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and inorganic phosphate [1]. Genetic and kinetic studies so far have demonstrated that at least two distinct isoenzymes of FBPase e
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br Acknowledgements We thank Kathy Spindler for
2021-11-25
Acknowledgements We thank Kathy Spindler for helpful review of the manuscript. Expert technical assistance from Joel Whitfield in the University of Michigan Cancer Center Immunology Core is greatly appreciated. This research was supported by the American Heart Association (16GRNT30250013) and by
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