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br Funding br Conflicts of interest br Acknowledgement br In
2020-08-06
Funding Conflicts of interest Acknowledgement Introduction We have previously cloned from fetal human brain a seven transmembrane domain receptor (Jazin et al., 1993a) which at that time had no known ligand or function. We showed that this receptor was expressed in several human neurobla
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The present results were unanticipated based on the majority
2020-08-06
The present results were unanticipated based on the majority of data in the literature. Instead of blocking the behavioral and biochemical correlates of anxiety, we found a significant, and in the case of ASV-30, dose-dependent, potentiation by CRF2 receptor antagonists of fear-stimulated rat freezi
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Expression levels of osteoclast markers such as TRAP and
2020-08-05
Expression levels of osteoclast markers, such as TRAP and cathepsin K mRNA, were also significantly reduced in the LPS and DPP-4 inhibitor co-administered group, compared with the LPS-administered group. Furthermore, we evaluated the inhibitory effect of DPP-4 inhibitor on LPS-induced bone resorptio
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Intriguingly McClean et al reported that when interacting wi
2020-08-05
Intriguingly, McClean et al. [37] reported that when interacting with DNA, quaternary N-mustard 4-anilinoquinolinium conjugates (Supplementary Figure S7) bind strongly to AT-rich sequences in the minor groove. It remains unclear why the 6,7-methylenedioxy-quinoline pharmacophore in SL-1 prefers layi
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Our previous studies have demonstrated that the DDR discoidi
2020-08-05
Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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br Conclusion In this study we provided data
2020-08-05
Conclusion In this study, we provided data for a fast on and fast off reversible pan-CYP inhibitor which has potent inhibition toward 7 major human CYPs. It is a good tool in drug discovery to differentiate the contribution of CYPs toward the total metabolism (e.g. conjugation or protein mediated
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A cocktail approach can detect the activities
2020-08-05
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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The ketogenic diet has modest efficacy in
2020-08-05
The ketogenic diet has modest efficacy in treating epilepsy in CDD. The largest cohort reported 104 individuals with CDD treated with median ketogenic diet duration of 17 months and reductions in seizure frequency in 61 of 104 (58.7%) individuals, consistent with data from the Boston Children\'s Hos
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The synthesis of the aziridine started
2020-08-05
The synthesis of the aziridine () started with -aspartic Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) as chiral building block. Methylation of the carboxylic acids followed by the introduction of the required sulfonamide yields the diester . The diester was then reduced to reveal diol wh
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This study focuses on mechanisms of reciprocity between
2020-08-05
This study focuses on mechanisms of reciprocity between DGTS and PC in fungi during Pi starvation. We report changes in expression of the BTA1 gene and two PC biosynthesis genes during phosphate starvation of F. velutipes culture. We describe the deduced amino Moxidectin australia sequence and geno
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The development and physiology of cartilage
2020-08-05
The development and physiology of cartilage and bones are highly similar in mammals and teleosts validating the zebrafish as a reliable vertebrate model in this field [22]. Expression of genes and the molecular pathways involved in the endochondral ossification are well conserved. For instance, as i
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Rheological durability and fresh properties of cement grouts
2020-08-05
Rheological, durability, and fresh properties of cement grouts are generally improved by using chemical and mineral admixtures. Adding GSK180 to the grout at different compositions changes the hardened and the rheological properties of grouts. For different kinds of grout applications different addi
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Rheological durability and fresh properties of cement grouts
2020-08-05
Rheological, durability, and fresh properties of cement grouts are generally improved by using chemical and mineral admixtures. Adding SU 5402 to the grout at different compositions changes the hardened and the rheological properties of grouts. For different kinds of grout applications different add
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(±)-Nutlin-3 australia E ubiquitin ligases are key play
2020-08-05
E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligases
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br Results and discussion The compounds listed in Table Tabl
2020-08-04
Results and discussion The compounds listed in Table 1, Table 2, Table 3 were tested for their binding affinity to the human CRF1 Genistein and antagonist activity in a CRF-stimulated adenylate cyclase assay. One of the leading compounds with higher receptor binding and antagonist activity was t
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