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The benzimidazole group seems to be
2023-10-07
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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br Phosphorylation of P c Initial studies
2023-10-07
Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor
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Moreover showed reduction in fibroblast growth factor
2023-10-07
Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (P summary, a series of potent dual inhibitors of Axl kinase and VEGF-R2 h
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Recent progress has been made in translating animal
2023-10-07
Recent progress has been made in translating animal findings on memory performance and amnestic effects – that are largely determined by tonically active receptors in which α5 contributes to the benzodiazepine binding site. Based on the observation that deletion of this subunit led to improved spati
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br The pathogenesis of AD and the targets
2023-10-07
The pathogenesis of AD and the targets of apelin Alzheimer's drugs Conclusions Introduction APJ, first identified from a human genomic library in 1993, belongs to a member of seven trans-membrane G protein-coupled receptor family. Its amino TAK-875 receptor sequence has 31% homology wit
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As with most G protein
2023-10-07
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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The increased occurrence of ARIA E in APOE carriers
2023-10-07
The increased occurrence of ARIA-E in APOE ε4 carriers in phase 2 studies resulted in separate protocols for carriers and noncarriers in the subsequent phase 3 studies. Two 18-month trials comprising 1121 carriers and 1331 noncarriers with mild to moderate AD tested doses of bapineuzumab that varied
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br Conclusion br Acknowledgement This study was supported by
2023-10-07
Conclusion Acknowledgement This study was supported by NIH/NINDSR01 NS036812-16. Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the gene
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salvinorin a The application of diuretics induce an increase
2023-10-03
The application of diuretics induce an increased rate of water exiting brain cells encouraging the formation of increased intracellular polyphosphoric acid. In the absence of the diuretic water is retained in cells converting polyphosphoric salvinorin a to monophosphoric acid. The latter change dec
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The purpose of this study is
2023-10-03
The purpose of this Vandetanib hydrochloride study is to examine the relationship between ACEs and engagement in treatment among a sample of youth in residential treatment centers (RTCs). It is hypothesized that youth with higher ACE scores will have lower levels of engagement in treatment. In orde
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The synthetic route to M developed by Rice was
2023-10-03
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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Prostate cancer is the second leading cause of cancer relate
2023-10-03
Prostate cancer is the second leading cause of cancer-related death in men in the United States [25]. Similar to pancreatic cancer, prostate cancer has few diagnostic options available, particularly to differentiate indolent from aggressive disease. Axl is also overexpressed in ∼50% of prostate canc
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Physiological total plasma LPA levels are normally less than
2023-10-03
Physiological total plasma LPA levels are normally less than 1μM in healthy subjects. LPA levels have been reported to be increased in malignant effusions or plasma in cancer patients [20]. In addition, increasing ATX activity detected in healthy pregnant women in the third trimester of pregnancy ex
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The LOX hydroxide metabolites are converted to secondary lip
2023-10-03
The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4
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Bamboo shoots with their high nutritive http www apexbt
2023-10-01
Bamboo shoots, with their high nutritive and therapeutic value, are now used for food fortification (Nirmala & Bisht, 2017). Several value-added products such as nuggets, crackers, chutney, snacks, cookies, cakes, chappaties, and buns have been prepared from bamboo shoots (Table 3). Dietary fiber fr
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