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The present study also showed that EP deficiency and EP
2021-04-17
The present study also showed that EP2 deficiency and EP4 antagonism significantly suppressed psoriatic TAK 165 mg in an imiquimod model. Notably, however, the combined EP2 deficiency and EP4 antagonism did not completely suppress ear swelling in this model, possibly because there is the IL-17–inde
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EP EP and EP receptor expression on
2021-04-17
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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Clodronate Disodium Previous studies demonstrated that cPLA
2021-04-17
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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Enzyme mimics belong to a type of rising catalysts which
2021-04-17
Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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(+)-Apogossypol Many studies have documented that enolase ac
2021-04-17
Many studies have documented that enolase acts as a plasminogen-binding protein and this interaction is involved in the tissue invasion and pathogenicity of the causative agents (Almeida et al., 2004; Avilan et al., 2000; Marcilla et al., 2007; Mundodi et al., 2008; Vanegas et al., 2007). Furthermor
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The pseudo DUBs KIAA and Abraxas are required for the
2021-04-17
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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br Results and discussion In the present study we used
2021-04-17
Results and discussion In the present study, we used a set of compounds (Fig. 2) consisting of ATP (a), dATP (b), an ATP analog containing β,γ-nonhydrolyzable hypophosphate P-P bond (c), and three pairs of P-diastereoisomers of α-thio-ATP analogs (d,e,f) containing a sulfur CT99021 instead of on
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br Introduction Diacylglycerol kinase DGK is a lipid metabol
2021-04-17
Introduction Diacylglycerol kinase (DGK) is a lipid-metabolizing enzyme that phosphorylates diacylglycerol (DG) to produce phosphatidic benfotiamine (PA) [[1], [2], [3], [4]]. DG and PA act as lipid second messengers in a wide variety of biological processes. Ten DGK isozymes (α, β, γ, δ, η, κ,
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DHODH activity has been traditionally measured with the stan
2021-04-17
DHODH activity has been traditionally measured with the standard colorimetric assay that monitors 2,6-dichloroindophenol (DCIP) reduction as absorbance decrease at 600 nm . This assay has permitted the identification of several families of DHODH inhibitors in a successful high-throughput screening (
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Moreover maintaining the pyrimidine pool is
2021-04-17
Moreover, maintaining the pyrimidine pool is not the only important role played by DHODHs. In Toxoplasma gondii, for instance, DHODH plays a second essential function [38] possibly coupled to the mitochondrial respiratory activity, where it replenishes ubiquinol levels and prevents reactive oxygen s
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The present study provides the
2021-04-17
The present study provides the first evidence that the human uroepithelial Heparin sodium in vitro respond directly, within 48h, to this carcinogen by promoting extensive vacuolation and DAPK expression. By using the TEM, ICC and Western blotting, we found that the arsenite-induced vacuoles were der
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It is now widely known that blockade of CysLT
2021-04-17
It is now widely known that blockade of CysLT1 receptors strongly inhibits antigen-induced bronchial contractions in specimens isolated from non-asthma subjects. However, this blockade is not complete as shown in the present study and in other literature.4, 15, 16 The results of the current study su
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During the course of our research on mGlu PAMs the
2021-04-17
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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CYP s are heme containing monooxygenases constituting a
2021-04-17
CYP450s are heme-containing monooxygenases constituting a conserved gene superfamily of heme-thiolate proteins, and are found in prokaryotes and eukaryotes (Martignoni et al., 2006). They play a key role in detoxification of endogenous (e.g., steroids) and exogenous compounds (e.g., drug, insecticid
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Midazolam oral clearance is used for characterization of
2021-04-17
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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