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br Acknowledgements We are grateful to the
2020-12-23

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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In some pancreatic and non pancreatic
2020-12-22

In some pancreatic and non-pancreatic tissues, the chloride and calcium channels are heavily regulated by phosphorylation by protein kinases, such as PKC, cyclic AMP-dependent protein kinase (PKA), PKCaMKII, PI3K and protein tyrosine kinases [7,36,37]. Since the interaction of triterpenes with recep
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br Conclusion The present work describes
2020-12-22

Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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L-365,260 australia Immune modulation by steroid hormones is
2020-12-22

Immune modulation by steroid hormones is a rather new aspect of the research on endocrine interactions in lower vertebrates (Harris and Bird, 2000). In the classical view, steroids exert their effects by binding to specific intracellular receptors that function as ligand-activated transcriptional re
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Estrogen related receptors ERRs are orphan nuclear
2020-12-22

Estrogen-related receptors (ERRs) are orphan nuclear receptors and have three members including ERRα, ERRβ, and ERRγ (Yasumoto et al., 2007). Though they are termed as ERRs due to the sequence homology with estrogen receptors, they don’t need to bind estrogens to exert action. Generally, ERRs bind t
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br Conclusions br Declaration of interest
2020-12-22

Conclusions Declaration of interest Acknowledgment This work was supported by an AIRC (Associazione Italiana Ricerca Cancro-Milan) Grant KFR062-2 to A.G.L, by Ricerca Funds by Fondazione IRCCS Ca’ Granda Ospedale Maggiore Policlinico (Grant No. 180/01) and by the ERA-NET “ERare” (Grant GO
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Molecular docking study of compound was
2020-12-22

Molecular docking study of A 967079 was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cyano-hyd
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Synthesis of and is described in Scheme Compounds and
2020-12-22

Synthesis of 5–7, 12–14, and 18 is described in Scheme 3. Compounds 5–7 and 18 were prepared as outlined in Scheme 3a. Reaction of 4-bromomethylbenzoic MPC 6827 hydrochloride (36) with thionyl chloride yielded the corresponding acid chloride, which was converted to the corresponding amide 40a by th
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Drug resistance to both pathogens
2020-12-22

Drug resistance to both pathogens and cancer has been a big hindrance in healthcare. Integrated research undertakings are being pursued to find the exact causes of the lack of response towards drugs. Surprisingly, host pumps are the key factors in failure of most drugs. The pumps either do not allow
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In human neuroblastoma SH SY Y cells and in
2020-12-22

In human neuroblastoma SH-SY5Y 2825 and in lymphoma Jurkat cells, Yamanaka et al. [56] showed that exogenously added 24(S)-hydroxycholesterol could be efficiently esterified by ACAT1. These results suggest that both ACAT1 and ACAT2 can control the oxysterol levels by directly esterifying them, in a
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br Materials and methods br Results br Discussion The
2020-12-22

Materials and methods Results Discussion The nitric oxide generating enzymes of the NOS family comprise three isoforms: nNOS, iNOS and eNOS [31]. Expression of eNOS is mainly found in endothelial Triptolide where it physically promotes vasodilation [32]. Conversely, evidence also indicates
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Axitinib Hyaluronic acid HA also called
2020-12-22

Hyaluronic Axitinib (HA), also called hyaluronan is widely distributed in Extra Cellular Matrix of soft connective tissues including skin, umbilical cord and synofial fluid (Hanamura et al., 2008). Hyaluronic acid has a unique ability to hold 6000mL of water in 1mg of HA and plays an important role
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Besides EGFR other tyrosine kinase receptors are currently g
2020-12-22

Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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While oxysterols were most extensively studied for its poten
2020-12-22

While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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Several main strategies for targeting
2020-12-22

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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