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Previous studies showed that many steroidogenic enzymes act
2020-11-02
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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ampa receptors In the course of our program which was
2020-11-02
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Given a disruption of membrane internalization and
2020-11-02
Given a disruption of membrane internalization and an increase in synaptic glutamate receptors in CPG2 knockdown neurons, one might expect an increase in dendritic spine size as membrane continues to be inserted into the spines during receptor exocytosis. However, we observed the opposite phenotype,
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Furthermore positioning the naphthalene nucleus in d within
2020-11-02
Furthermore, positioning the naphthalene nucleus in 3d within the main active site and forming one hydrogen bond with Tyr385 in addition to many hydrophobic interactions with Val349, Leu352, Gly526, Ala527 and Leu531 residues, correlates well with the position and hydrophobic interactions of the tri
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Autophagy is a dynamic process
2020-11-02
Autophagy is a dynamic process that primarily involves autophagosome formatting and lysosomal degradation, and these processes are controlled by autophagy-related genes (Atg) (Klionsky et al., 2012). The related protein SQSTM1/p62 (sequestosome 1) importantly serves as a signalling director in sever
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br Acknowledgements We are grateful to the National
2020-11-02
Acknowledgements We are grateful to the National Natural Science Foundation of China (Grant Nos. 21571033 and 81503099) and the New Drug Creation Project of the National Science and Technology Major Foundation of China (Grant No. 2015ZX09101032) for financial aids to this work. The research was a
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SH-4-54 synthesis p and p which are downstream of pAkt and
2020-11-02
p21 and p16, which are downstream of pAkt and pERK1/2, are tumor suppressors which induce cell senescence and SH-4-54 synthesis arrest [[56], [57], [58]]. Inhibitors of pAkt or pERK1/2 can activate p21 and p16 and promote cell senescence and cell cycle arrest [11,12,[59], [60], [61]]. It is well kn
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To develop novel EPAC inhibitors
2020-11-02
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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The imbalance that renders greater lipid uptake
2020-10-31
The imbalance that renders greater lipid uptake toxic is unclear, but the comparison of our in vitro studies with those in mice illustrates the importance of TAG storage versus accumulation of less non-polar molecules. Protective effects of ACSL1 and PPARγ have been reported in other cell types. Par
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In contrast DAG phosphorylation to PA
2020-10-31
In contrast, DAG phosphorylation to PA by diacylglycerol kinases (DGKs) represents a quantitatively minor metabolic pathway, but is generally regarded as a main disposal pathway for “signaling” DAG. PA produced by DGKs is an intermediate of the synthesis of CDP-DAG, cardiolipin and PI. However, PA i
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Previous studies from our lab looked at the
2020-10-31
Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to ide
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In the present study we combined
2020-10-31
In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis SQ 22536 and leaves, we demonstrate that this sub-class of plant proteases is activated in resp
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Other karyopherins besides CRM must bind
2020-10-31
Other karyopherins besides CRM1 must bind to FG-Nups in a similar fashion. However, at an atomic resolution, only the interaction of importin β with isolated FG motifs has been analyzed (Bayliss et al., 2000, Bayliss et al., 2002, Liu and Stewart, 2005). Despite similarities in the FG-binding pocket
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The proposed FDIR technique is
2020-10-31
The proposed FDIR technique is presented in the following format: Section 2 contains a survey of typical orbits of interest with regard to the AS1842856 environment found in them, which is contrasted with a LEO orbit. Additionally, how the requirements for the satellite system can be estimated is p
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Materials and methods Construction of the Chk YB b Neo
2020-10-31
Materials and methods Construction of the Chk-YB-1b-Neo vector. Approximately 107 plaques from a chicken genomic library established in EMBL3 vector (Clontech Palo Alto, CA) was screened and one clone containing a 12kb insert was selected. Digestion of this clone with SalI and EcoRI restriction enz
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