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Classical drugs target the viral
2022-06-15
Classical drugs target the viral protein kinase inhibitor reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has be
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MK cyclobutylpiperidin yl oxyphenyl methyl
2022-06-15
MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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bromophenol blue br Materials and methods br Results br Disc
2022-06-15
Materials and methods Results Discussion Accurate HER2 assessment for patients with invasive breast cancer is crucial to determining which patients may benefit from HER2-targeted therapy. The most recent ASCO/CAP guidelines have again redefined HER2 gene amplification as determined by dual-
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Renal disease is characterized by aberrant fibrotic
2022-06-15
Renal disease is characterized by aberrant fibrotic remodeling of renal tissue, elevated apoptosis in kidney tissue, and eventual organ failure. In addition, patients with renal disease are more likely to suffer from systemic hypertension due to oxidative damage (reviewed in Ref. [18]). Treatment of
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br Materials and methods br Results br Discussion In this
2022-06-14
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the L-Cysteinesulfinic acid coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprina
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The treatment target which aims
2022-06-14
The “90-90-90 treatment target” which aims at diagnosing 90% of HIV-infected individuals, treating 90% of those diagnosed and achieve viral suppression for 90% of treated individuals, is a key strategy to achieve one of the sustainable development goals (SDG) of ending AIDS as a public health threat
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The average pregnancy rate in
2022-06-14
The average pregnancy rate in this work was 60.1%; similar results have been reported with the same estrus synchronization treatment (58% pregnancy rate) [26]. Later studies also showed that the pregnancy rate was 56.9 and 51.1%, with FTAI and estrous detection, respectively [34,35]. Although that t
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It is essential to maintain genome integrity
2022-06-14
It is essential to maintain genome integrity and stability which is assaulted by oxidative stress. To perform this function, all human cells have well developed repair systems. Base excision repair (BER) system is the most effective pathway responsible to revert back lesions caused by oxidative stre
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Heparin and suramin are highly negatively
2022-06-14
Heparin and suramin are highly negatively charged molecules, and they are in this aspect, similar to DNA and likely to compete with DNA by binding to the protein cationic groups [17] (Fig. 1). The inhibitory effect of heparin and suramin on DNA and RNA binding proteins has been described [[18], [19]
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roscovitine In conclusion we have designed and characterized
2022-06-14
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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ATP is essential for maintaining the ionic balance of
2022-06-14
ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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br Acknowledgements br Introduction High
2022-06-14
Acknowledgements Introduction High-intensity noise exposure has long been known to induce damage in the peripheral and central auditory system, often resulting in auditory pathologies such as hearing loss, tinnitus and hyperacusis (Syka, 2002; Roberts et al., 2010). Within the inner ear, struc
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The first FPR ligand described is
2022-06-14
The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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Sensitivity to EphB TKI was also
2022-06-14
Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 1478 after transient transfection of pCMV6-AC-GFP/EphB3, and both were demonstrated to be
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In this study we intended to explore the efficacy of
2022-06-14
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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