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br Introduction Biocatalysis can be used to
2021-08-11
Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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Similarly LTD concentration dependently enhanced AQP express
2021-08-10
Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current
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During the course of our research on mGlu
2021-08-10
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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In the course of our program which
2021-08-10
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Finally unilateral microinjection of CP Astressin B CP CRF
2021-08-10
Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, AN
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Preparation of the pyridyl ether analogs
2021-08-10
Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate, fo
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br Diseases which have been
2021-08-10
Diseases which have been treated with proteins linked to HSA A number of therapeutic products conjugated to HSA have now been approved for clinical use (Table 2). For example, fatty dna ligase derivatives of human insulin bound to HSA have applications in the treatment of diabetes while paclitax
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Though limited to a large cohort of self reported healthy
2021-08-10
Though limited to a large cohort of self-reported healthy individuals, associations between individual purinergic receptors have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-predicted
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Our results for imidacloprid were
2021-08-10
Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic o6 methylguanine methyltransferase receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes
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IAA sensitive Cl channels were shown to mediate
2021-08-10
IAA-94-sensitive Cl channels were shown to mediate cardioprotection due to IPC (Diaz et al., 1999) and cyclosporine A (Diaz et al., 2013). CLIC-like channel activity was also observed in cardiac mitoplast (Misak et al., 2013) but the molecular identity of these intracellular Cl channels and their pr
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Role of ROS signaling in regulating cell
2021-08-10
Role of ROS signaling in regulating cell death pathways has been well established. Involvement of CLIC1 in ROS production has been studied earlier. It was observed that macrophages from clic1 mice showed ~30% decrease in cellular ROS generation which effects macrophage function (Jiang et al., 2012).
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Our observation that nuclear but not cytoplasmic
2021-08-10
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant tbtu australia whereas cytoplasmic EP4 was commonly observed [13]. While G protein-coupl
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Previously we have described increased
2021-08-10
Previously, we have described increased expression of both cytokine and chemokine mRNA (e.g. MCP-5 and fractalkine) in the left ventricle of male EP4-KO mice with dilated cardiomyopathy [2]. Takayama et al. [31] have shown that PGE2 potently inhibits cytokine/chemokine secretion (MCP-1, interleukin
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We elucidated that the ten DGK
2021-08-09
We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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The sixth affected individual individual is a year
2021-08-09
The sixth affected individual (individual 6) is a 35-year-old female who presented with a complex combination of congenital and acquired symptoms. She was born to healthy, unrelated parents with an unremarkable family history, apart from the presence of polycystic kidney disease in her father and pa
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