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In general FPSs require Mg or Mn as a cofactor
2022-02-21
In general, FPSs require Mg2+ or Mn2+ as a cofactor for GPP and FPP synthesis. Co2+ also acts as a cofactor in EuFPSs, as in the case for PcFPS and Abies grandis FPS [29], [44]. Co2+ enhanced the activity of EuFPS1 more than the activity of EuFPS2: Mg2+, Mn2+ and Co2+ had approximately the same effe
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br Materials and methods br Results br Conclusions In
2022-02-21
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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VDAC interacts with hexokinase and is implicated in
2022-02-21
VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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According to the experimental data HKI preferentially binds
2022-02-21
According to the experimental data, HKI preferentially binds to the mitochondrial inter-membrane contact sites formed by ANT and VDAC [[5], [6], [7],27], mainly via the VDAC1 isoform [7,8]. These electrogenic contact sites allow application of a part of IMP to MOM by transferring phosphoryl groups f
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An important example of a
2022-02-21
An important example of a frame is the lattice of open subsets of any topological space X. The correspondence is clearly functorial (by taking inverse images), and consequently one has a contravariant functor with the category of topological spaces and continuous maps as domain category. The functor
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br Hh Proteins at a Glance Hh family
2022-02-21
Hh Proteins at a Glance Hh family proteins are evolutionarily conserved morphogens that provide cells with positional information and fate instruction during early embryonic development. After development, Hh ligands contribute to tissue homeostasis and wound healing 1., 2.. Consistent with these
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Considering that TGF plays a pivotal
2022-02-21
Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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br Ethical approve and consent to participate br Consent for
2022-02-21
Ethical approve and consent to participate Consent for publication Availability of supporting data Competing interests Funding This work was supported by a grant from Key Program of National Natural Science Foundation of China (No. 81330089) and the Shanghai Science and Technology Fun
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Substrate affinity and specificity can
2022-02-21
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of MDL 28170 bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of shor
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As GSH cellular redox status is critical for various biologi
2022-02-21
As GSH cellular redox status is critical for various biological phenomena including apoptosis and inflammation [34], [35] we hypothesized that inflammation could modulate GSTP1-1 gene expression. Indeed, reactive oxygen species (ROS) are released at inflammation sites and can be eliminated from hyPe
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pfk The number of small molecule GSK inhibitors is continuou
2022-02-21
The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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Given the involvement of dysregulated S nitrosylation in
2022-02-21
Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the
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br Positive regulation of gene expression by Nrf br
2022-02-21
Positive regulation of gene aromatase inhibitors by Nrf2 Repression of Nrf2 by Keap1 Because many xenobiotic inducers of NQO1 and GST enzyme activities contain a thiol-reactive electrophilic moiety (i.e. are soft electrophiles), Paul Talalay and colleagues predicted in 1988 that they would be
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br Acknowledgments We thank Dr Kathleen Sullivan of Merck
2022-02-21
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 fda approved mg expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. An
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For the study described herein analogues of CID were
2022-02-21
For the study described herein, analogues of CID1792197 (2) were selected for exploration. There are a variety of reasons for this decision. First, the synthetic approach, described hereafter, is modular in nature to rapidly enable the independent modification of either end of the molecule. Second,
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