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The compounds f and a
2022-08-22
The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pote
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br Acknowledgement br Introduction Malignant melanoma is an
2022-08-22
Acknowledgement Introduction Malignant melanoma is an aggressive and highly metastatic cancer. The incidence of malignant melanoma is increasing all over the world, and the population of patients with advanced melanoma is growing [1], [2]. Malignant melanoma is often resistant to conventional
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Furthermore increased plasma levels of endoglin have been
2022-08-22
Furthermore, increased plasma levels of endoglin have been associated with diabetic complications (Valbuena-Diez et al., 2012). The involvement of soluble endoglin in a number of widespread pathologies demonstrates that endoglin is not only marker of endothelial integrity but also a causative factor
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Among the symbiotic bacteria contained in
2022-08-22
Among the symbiotic bacteria contained in the probiotics, lactic-acid-producing bacteria (LAB) have been suggested to confer broad spectrums of health benefits, such as activation of mucosal and systemic immunity and resistance to infectious illnesses (Schiffrin et al., 1995, Wells and Mercenier, 20
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Typically upon chronic agonist exposure GPCRs undergo desens
2022-08-22
Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have
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AFB Fapy dG has been
2022-08-22
AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by K-Ras(G12C) inhibitor 12 excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1
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Among the various delivery strategies in the field
2022-08-22
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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Introduction The brain contains abundant
2022-08-22
Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev
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It is increasingly argued that the
2022-08-22
It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit SMER 3 of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with the idea that GC-mediated repression
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The observed CORT induced increase in Cx phosphorylation at
2022-08-22
The observed CORT-induced increase in Cx43 phosphorylation at S368 may also contribute to GJIC disruption. Gap junction channel permeability is modulated through connexin phosphorylation (Moreno and Lau, 2007). Specifically, the phosphorylation of Cx43 on S368 has been previously shown to decrease i
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Based on the above considerations
2022-08-19
Based on the above considerations, the β-galactosidase gene from Exiguobacterium acetylicum MF03 (not previously reported) was cloned, expressed and purified with the aim of assessing the potential of this novel enzyme for catalyzing reactions of synthesis and hydrolysis of glycosides. Because of E.
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In fish little information about Gpr is available We have
2022-08-19
In fish, little information about Gpr84 is available. We have revealed that lipopolysaccharide (LPS) induces significantly up-regulation of zebrafish , and zebrafish overexpression markedly increased the LPS-stimulated production of the cytokine []. Here we expanded on these studies to further inv
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phorbol 12 myristate 13 acetate receptor The normal function
2022-08-19
The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa
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To understand the structural basis for the mode of action
2022-08-19
To understand the structural basis for the mode of action of indole-based compounds the crystal structures of bound to both the wild type and A128T IN CCDs have been solved. The X-ray crystallography studies have revealed that binds at the IN dimer interface in the principal LEDGF/p75 binding pock
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Introduction Pneumocystis pneumonia PCP is a respiratory
2022-08-19
Introduction Pneumocystis pneumonia (PCP) is a respiratory invasive infection caused by Pneumocystis jirovecii, an ubiquitous fungus. It is transmitted by air and mostly infects immunocompromised patients. PCP is characterized by respiratory complaints of cough, dyspnea, but also tachycardia, low g
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