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The ability of minor groove
2020-09-01
The ability of minor groove binding agents to inhibit the activity of DNA helicases is not without precedence. Similar effective inhibition of the unwinding of DNA by the BLM and Werner\'s DNA helicases by the minor groove binder distamycin A has been observed. Further, and similar to RecBCD, interc
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br Allosteric inhibitors In general candidate drugs that
2020-08-31
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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br Experimental procedures br Acknowledgments br Introductio
2020-08-31
Experimental procedures Acknowledgments Introduction Receptor tyrosine kinases (RTKs) control many fundamental cellular processes, such as cell proliferation, differentiation, migration, and metabolism (Lemmon and Schlessinger, 2010). RTK activity is normally tightly controlled, and dysregu
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To further define the importance of CYP
2020-08-31
To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H
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In the signaling cascade of innate immunity
2020-08-31
In the signaling cascade of innate immunity, most of the receptor proteins, adaptor proteins, and kinases are modified by ubiquitination to activate and transduce the downstream signaling for efficient production of the IFN and proinflammatory cytokines to combat the pathogens. For example, the K-63
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The pseudo DUBs KIAA and
2020-08-31
The pseudo DUBs KIAA0157 and Abraxas are required for the catalytic function of BRCC36. Comparison of the BRCC36–KIAA0157 heterodimer structure with an inactive BRCC36 homodimer structure provides a model for understanding how this functional interplay is achieved. As shown in schematic form in Figu
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As previously reported azole class
2020-08-31
As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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Our results show that COX
2020-08-31
Our results show that COX-1 and COX-2 inhibition improve cognitive performance and decrease the neuronal insult during HH. However, when a neuroinflammatory response was observed, COX-1 inhibition was more effective than COX-2 inhibition at reducing microglial activation and augmenting pro-inflammat
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br Material and methods br Results br
2020-08-31
Material and methods Results Discussion A. fumigatus utilizes several virulence factors that facilitate its establishment in human hosts. Among these factors, the best known are hydrolytic enzymes such as proteases and phospholipases, toxins, melanine and catalases that neutralize the react
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br Material and methods br Results br Discussion
2020-08-31
Material and methods Results Discussion Isolated PD173955 synthesis have several potential advantages over other in-vitro approaches, such as expression of properties similar to their site of origin including the possibility of bidirectional transmembrane transport and exposure. Furthermor
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sc9 br NF B and STAT as Regulators of the CDK
2020-08-28
NF-κB and STAT as Regulators of the CDK System While current data support the concept that CDKs augment the proinflammatory activity of NF-κB, our understanding of the function of this transcription factor system in CDK regulation remains patchy. Seminal studies showed the contribution of NF-κB t
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Nile tilapia Oreochromis niloticus is an important species
2020-08-28
Nile tilapia (Oreochromis niloticus) is an important species farmed worldwide (Doan et al., 2018). Lipid-rich diets are commonly used in Nile tilapia aquaculture to reduce feed cost, but impair lipid homeostasis (Huang et al., 2016). Therefore, it is important to determine whether forskolin can stim
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Early tubular differentiation in WT lacks lumen formation
2020-08-28
Early tubular differentiation in WT lacks lumen formation and, therefore, sometimes can be confused with rosettes of ES/PNET or neuroblastoma. However, tubular structure usually has Bikinin neatly aligned to form a single layer around the future lumen, whereas neuroblastic rosettes are arranged mor
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br Introduction Cancer related inflammation
2020-08-28
Introduction Cancer related inflammation is associated with poor prognosis and reduced survival in numerous human malignancies. Expansion of myeloid derived immune 1530 synthesis in response to tumor-secreted factors largely contributes to the heightened systemic and intra-tumoral inflammatory m
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Nimodipine administration also inhibited the eIF ATF singnal
2020-08-28
Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s
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