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Epigenetic drugs such as HDAC inhibitors regulate
2021-09-18
Epigenetic drugs, such as HDAC inhibitors, regulate gene expression by affecting the activity of histone or DNA modifying enzymes and their associated transcriptional response [141]. BET bromodomain protein inhibition is another epigenetic approach for blocking the Hedgehog pathway at the downstream
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Of what interest is the link between GSNOR
2021-09-18
Of what interest is the link between GSNOR and NO in the plant response to Fe deficiency? On the one hand, NO acts as an important signal to help plants accommodate Fe deficiencies; on the other hand, surplus NO is indeed a harmful RNS that induces severe S-nitrosylation-related damage at a higher s
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To gain insights for further improvement of the agonistic ac
2021-09-17
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocycli
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The occurrence of MDR in
2021-09-17
The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer Digoxigenin-11-dUTP in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems includ
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Na K ATPase adenosine triphosphate ATP and astrocytic
2021-09-17
Na+/K+-ATPase, Zacopride hydrochloride and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increase
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br Acknowledgements This work was
2021-09-17
Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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Therefore as it stands presenilin
2021-09-17
Therefore as it stands, presenilin has a γ-secretase-independent role in regulating protein trafficking, proteolysis and degradation, however given that inhibition of γ-secretase activity can have a negative effect on protein trafficking [69], [98], we cannot exclude the possibility that some of the
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br Discussion br Author Contributions br Alzheimer s
2021-09-17
Discussion Author Contributions Alzheimer’s disease (AD) is an age-related, chronically progressive neurodegenerative disorder affecting more than 35million people worldwide and an estimated 5.5million in the US. Current marketed drugs such as acetylcholinesterase inhibitors and the NMDA ant
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A single ICV injection of
2021-09-17
A single ICV injection of GALP stimulated food intake in goldfish at 1h post-administration. This result is similar to that observed in rats, where ICV injection of GALP exerted an acute orexigenic effect [14], [15], [16]. Simultaneously, our findings counter the results found in mice, where central
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Also a large number of small molecules
2021-09-17
Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [
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In addition to the four
2021-09-17
In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i
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Thioguanine FXa is a vitamin K dependent serine
2021-09-17
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Thioguanine and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The ac
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br Acknowledgement The work was supported by
2021-09-16
6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors
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br Materials and methods br Author
2021-09-16
Materials and methods Author contributions Acknowledgments We thank members of the Skaar laboratory for critical evaluation of the manuscript. This work was supported by grants from the National Institutes of Health, R01AI069233 (EPS), and T32GM008554-21 (LJL). Introduction Pseudomonas
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Racemic protein crystallography has been
2021-09-16
Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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