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Some pyrimidine analogs are substrate
2020-04-02
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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br Results br Discussion Thus the
2020-04-01
Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh
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As discussed in the introduction many pregnant women take
2020-04-01
As discussed in the introduction, many pregnant women take medications such as nifedipine and indinavir, which are considerably metabolized by CYP3A [26]. Previous reports have also shown increased CYP3A activity following pregnancy [7], [9], which is consistent with our results. However, previous s
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The enzyme cyclooxygenase COX or
2020-04-01
The enzyme cyclooxygenase (COX) or prostaglandin endoperoxide H synthase (PGHS) is the key enzyme in the conversion of arachidonic chemokine receptor antagonist (AA) into prostaglandins (PGs) [1]. In 1991, researchers found that there were two isoforms of this enzyme called COX-1 and COX-2 with ind
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br Materials and methods br Results and
2020-04-01
Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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In contrast to SQLE HMGCR could be efficiently
2020-04-01
In contrast to SQLE, HMGCR could be efficiently degraded in Rifaximin synthesis lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our
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Haj Yahya et al applied native chemical ligation
2020-04-01
Haj-Yahya et al. [52] applied native chemical ligation for the construction of diubiquitin probes. They attached a cysteine residue to the lysine side chain of the proximal ubiquitin and ligated the distal module using the C-terminal thioester of ubiquitin. Elimination of the sulfur Vincristine sulf
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We also discovered important clues to
2020-04-01
We also discovered important clues to domain HBC of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs. Altho
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Illumina for 5 ng DNA Introduction Cytochrome P CYP A is the
2020-04-01
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The Illumina for 5 ng DNA level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and t
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Regarding the mechanism of action of CRF several studies
2020-04-01
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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CD is a key co stimulation surface marker that can
2020-04-01
CD28 is a key co-stimulation surface marker that can be detected in all peripheral T MI-773 receptor in newborns, and the proportion of CD28bearing T cells reduces progressively with age [reviewed by (Fagnoni et al., 1996; Weng et al., 2009)]. Therefore, CD28nullCD8+ T cells are one of the most ack
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In summary A is a potent orally available
2020-04-01
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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br Roles of ERR in Physiology and Disease br
2020-04-01
Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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One possible pitfall of using EPAC activators in the treatme
2020-04-01
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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Abdominal aortic aneurysm AAA is
2020-04-01
Abdominal aortic aneurysm (AAA) is considered a major health concern and is associated with extremely high rates of mortality in case of aortic rupture. The main pathophysiologic mechanisms leading to aortic dilation include the degradation of the extracellular matrix (ECM) components, such as colla
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