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In the Medicines for Malaria Venture MMV distributed the
2021-11-25

In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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br Materials and methods br Results
2021-11-25

Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka
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Aberrant expression of HKII may be a required
2021-11-25

Aberrant expression of HKII may be a required feature for cancer development and progression. Overexpression of HKII has been reported in tumor tissues of cancer patients with liver [9], ovary [8], [24] and larynx [25]. The clinical significance of HKII in cancer was noted as overexpression of HKII
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nigericin br Material and methods br Results br Discussion
2021-11-25

Material and methods Results Discussion In vitro testing is necessary to study DAA activity and putative RASs. Compared to enzymatic assays and replicons, HCV infectious culture systems reflect the full viral life cycle and previous results in these systems reflected clinical data.[13], [14
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br Substrate Interactions Outside of the Catalytic Cleft As
2021-11-25

Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use
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Whereas binding of activated RhoA to the
2021-11-25

Whereas binding of activated RhoA to the PH domains of the RhoGEFs is proposed to mediate positive feedback regulation (Chen et al., 2010b, Medina et al., 2013), the sequestration of p190RhoGEF by activated Rac1 reveals a novel putative physiological role, that is to utilize Rac1 to directly drive r
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Ras small GTPases are critical molecular switches that conne
2021-11-25

Ras small GTPases are critical molecular switches that connect extracellular signals to intracellular signaling pathways initiated by membrane receptors, such as growth factor receptors and G protein-coupled receptors (Simanshu et al., 2017). When shifting between active GTP-bound and inactive GDP-b
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Having identified initial leads and further
2021-11-24

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic TDZD-8 derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chloro and C
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The Bcl and Bcl xL genes contain the
2021-11-24

The Bcl-2 and Bcl-xL genes contain the CRE binding site in their promoter regions for CREB and CBP to bind to, so CREB phosphorylation was shown to up-regulate these anti-apoptotic genes, Bcl-2 and Bcl-xL [[29], [30], [31]]. Bcl-2 and Bcl-xL prevent the activation of caspases and the release of mito
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br Materials and methods br Results br
2021-11-24

Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 DCC-2036 sale has been identified within discrete regions of the ner
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GLP is known to be expressed in a subset
2021-11-24

GLP-1 is known to be expressed in a subset of taste bud cells and has been shown to co-localize with GPR120 in the circumvallate papillae [22]. Local GLP-1 regulates taste preference for sucrose [54]. Analogous to intestinal mediation of GLP-1 by GPR120, Martin et al.[22] report induction of GLP-1 s
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Recent studies suggested that non coding
2021-11-24

Recent studies suggested that non-coding RNAs participate in the modulation of Glut1 expression. For instance, the lncRNA NBR2-Glut1 axis was suggested to modulate cancer cell sensitivity to phenformin [37]. In renal carcinoma, miR-1291 is involved in the regulation of Glut1 TCS 2002 [38]. Therefore
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Yeast two hybrid screening studies have
2021-11-24

Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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Besides its established insulinotropic actions GIP has been
2021-11-24

Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M
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The intestinal epithelium is the first line of
2021-11-24

The intestinal epithelium is the first line of defense against pathogens and noxious agents and exerts a range of physiological activities, including digestion and 2-APB of nutrients. The intestinal wall consists of a series of finger shaped protrusions called villi and invaginations known as crypt
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