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The most potent compounds within the current
2023-01-04
The most potent compounds within the current series of compounds were therefore , , , , and , with Florfenicol possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-OHase
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LPA binds to six specific cell surface
2023-01-04
LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino gaba receptor agonist homology) An et al., 1997,
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Bilirubin synthesis Roles of Aurora kinases in
2023-01-04
Roles of Aurora kinases in directly activating multiple oncogenic pathways and promoting proliferation as well as transformation have also been demonstrated. Aurora-A has been shown to up-regulate telomerase reverse transcriptase mRNA through c-myc [26]. The kinase was also implicated in activating
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Mitochondria are key organelles involved in
2023-01-04
Mitochondria are key organelles involved in the mechanism of apoptosis (Xiong et al., 2014), and loss of ΔΨm is an important marker associated with mitochondrial dysfunction and cell death. We found that Mino induced ΔΨm impairment and nuclear fragmentation in Jurkat SP 141 in a concentration-depend
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Our observation that squalestatin caused only small
2023-01-04
Our observation that squalestatin caused only small differences in the production of Aβ40 and Aβ42 was in contrast to prior reports of the effects of other cholesterol synthesis inhibitors. This may be due to using squalestatin, a more specific cholesterol synthesis inhibitor that does not affect is
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We designed SSOs that block
2023-01-04
We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 tak 242 including the γ-secretase cleavage sites that give rise to the toxic, AD-associated Aβ42 pep
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Some of the earliest LOX inhibitors were redox inhibitors in
2023-01-04
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic Cy5 TSA Fluorescence System Kit (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+)
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Several enzymes in serine and glycine
2023-01-04
Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a
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A 205804 australia Ultraviolet UV spectroscopy is commonly
2023-01-04
Ultraviolet (UV) spectroscopy is commonly used for screening potential ADA inhibitors [15]. In the UV method, the ADA reaction is calculated by measuring the decrease in absorbance of the substrate at 265 nm or increase in absorbance of the product at 248 nm. However, AD and inosine share a very clo
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Introduction Dementia is a common disease in
2023-01-02
Introduction Dementia is a common disease in the elderly, and a significant source of disability, healthcare spending, and long-term care admissions. There is evidence to suggest that testosterone plays a role in cognitive functioning, and lower serum levels correlate with higher amyloid deposits (
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Aurora A overexpression is also related to
2023-01-02
Aurora-A overexpression is also related to the activation of NF-κB, a potent anti-apoptotic effector that may play a role in preventing apoptosis in cancer 5-ht2 [18]. These data show that we are still at the beginning of unraveling the complex mechanism by which these gene products and proteins i
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With regard to the first question subcellular fractionation
2023-01-02
With regard to the first question, subcellular fractionation studies revealed that BDK and PPM1K are clearly detectable in both the mitochondrial and cytosolic subcellular fractions, thus making it possible for these enzymes to interact with both the BCKDH and ACL substrates. The preferential presen
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br Conflict of interest statement br Acknowledgments
2023-01-02
Conflict of interest statement Acknowledgments Introduction Cellular responses to genotoxic stress in eukaryotic cells are coordinated by members of the phosphoinositide kinase related protein kinase (PIKK) family. Two members of this family, Ataxia–Telangiectasia mutated (ATM) and ATM and
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Introduction Cytochrome P CYP aromatase catalyzes the conver
2023-01-02
Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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Researchers demonstrated that mitochondria are
2023-01-02
Researchers demonstrated that mitochondria are the main producers of ROS and are the most sensitive to the effects of ROS. Mitochondria-mediated apoptosis may not be limited to the role of cytochrome c in the activation of caspase-3 and ROS may provide an alternate mitochondrial signaling pathway (
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