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Several studies have also shown that
2021-10-19

Several studies have also shown that HK2 may be an important downstream Polymyxin B sulfate of the PI3K/AKT/mTOR signaling pathway and may contribute to the development of cancer [15]. In our previous study, we found AKT2 expression was positively correlated with HK2 expression in primary colon can
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Polyphyllin VII Intestinal epithelium renewal is tightly con
2021-10-19

Intestinal epithelium renewal is tightly controlled by Hedgehog genes. Three Hedgehog genes are highly conserved in mouse and human, including Sonic hedgehog (Shh), Indian hedgehog (Ihh), and Desert hedgehog (Dhh) [13]. Hedgehogs bind to Patched (PTCH) [[14], [15], [16]], which unlike conventional r
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The endocytic inhibitors MDC and
2021-10-19

The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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Based on work from our
2021-10-19

Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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Glial cells have emerged as
2021-10-19

Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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Introduction Adaptations in the metabolism of cancers
2021-10-19

Introduction Adaptations in the metabolism of cancers contribute to tumor survival and growth and present opportunities to develop novel therapeutic strategies (Kelloff et al., 2005, Som et al., 1980). In particular, glutamine metabolism plays such an important role in cancer growth that a phenomen
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We recently reported the first cyclopropene analog of
2021-10-19

We recently reported the first cyclopropene-analog of the amino Boc-Phe-Osu receptor neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworker
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To further investigate if GPR was the functional target
2021-10-19

To further investigate if GPR40 was the functional target of these phenylpropiolic Dehydroandrographolide analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15].
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br Conclusion br Conflict of
2021-10-19

Conclusion Conflict of interest Acknowledgments This work was supported by an NRF grant (2016R1A2B4011196) from the Korea Research Foundation. Introduction Thymic epithelial tumors are rare, but they are the most common primary neoplasm of the thymus and of the anterosuperior mediastinu
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The expression of GLUT receptors
2021-10-19

The expression of GLUT receptors throughout the body could be considered a potential source for off-target effects even for engineered glucose-conjugated nanomedicines, as there are at least 12 types of GLUT transporters in the body, including GLUT1 in erythrocytes and the blood-brain barrier, as w
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Over the last decade intense
2021-10-18

Over the last decade, intense efforts have been devoted toward identifying IN inhibitors as potential drugs against HIV. Raltegravir and elvitegravir are integrase strand transfer inhibitors (INSTIs) that have been approved for therapy and dolutegravir is another INSTI that is currently in advanced
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Following the discovery of diketo compounds S and L
2021-10-18

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent cpi 1 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioassay
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Dithiodipyridine also known as aldrithiol
2021-10-18

2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency sh4 mg type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamine dihydrochloride s
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Chlorogenic acid The components of the SAGA complex includin
2021-10-18

The components of the SAGA complex including Gcn5 have recently been found to be involved in regulating pathways that are required for development and virulence in different species under the environmental stresses, around 10% of S. cerevisiae genes are activated by the transcriptional coactivator S
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Recently it has been found that treatment of human phagocyti
2021-10-18

Recently, it has been found that treatment of human phagocytic EPZ031686 or microvascular endothelial cells with NO donors inhibited the O2− generating capacity of NADPH oxidase [[8], [9], [10], [11]], which may involve down-regulation or S‑nitrosylation of the p47phox subunit (a cytosolic subunit
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