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Losmapimod br Results and discussion br Conclusion
2024-06-26

Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic Losmapimod group extending from the C-3 position of the aniline and substituted grou
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The identification of novel kinase inhibitor scaffolds is hi
2024-06-26

The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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br HMG proteins mobile modulators
2024-06-26

HMG proteins: mobile modulators of chromatin structure and cellular phenotype The term “High Mobility Group” was originally coined for the HMG proteins because of their unusual solubility properties, their small size and their rapid mobility, relative to other chromatin proteins, during gel elect
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Most of the latest http www
2024-06-26

Most of the latest works reported that in human hair follicle AR expression is restricted to DPC and is not found in the outer root sheath (ORS), hair bulb or bulge (Itami et al., 1995a, Jave-Suarez et al., 2004, Kariya et al., 2005, Pelletier et al., 2004, Thornton et al., 2003). DPC derived from b
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When arachidonic acid is used as
2024-06-25

When arachidonic UO126 is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy derivative. The r
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The G R mutation is located at the solvent front
2024-06-25

The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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These results validate the docked pose
2024-06-25

These results validate the docked pose of the ALR2-3e complex in comparison to the docked complex of the ALR2-4c complex of which the compound docked completely out of the binding pocket of ALR2 (). This concludes to that the removal of the acetic hsp90 inhibitors moiety leads to inactive or weakl
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Various compounds have been designed
2024-06-25

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic Imiquimod hydrochloride moiety, for example, 3-thiazolidineacetic acid derivative, which has been reporte
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In addition to it we
2024-06-25

In addition to it, we also showed that glycine increases miR-301a expression which directly binds to PTEN 3′UTR target sites [13]. Glycine confers neuroprotection through microRNA-301a/PTEN signaling in rats cortical neurons in oxygen deprivation model [13]. Substantial studies indicate that inhibit
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br Introduction Psychostimulant abuse and addiction remain a
2024-06-25

Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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br Actin at presynapses br Conclusion Thanks to the
2024-06-25

Actin at presynapses Conclusion Thanks to the recent discovery of rings, hotspots and trails, axonal lactacystin synthesis is back in the spotlight. These are exiting times for neuronal cell biologists armed with constantly improving labeling and imaging techniques to observe, quantify and pe
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Encouraged by this observation a systematic SAR study on
2024-06-25

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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Very recently Niessen et al
2024-06-25

Very recently, Niessen et al. have described the resensitizing effect of MB327 on nAChR performing solid-supported membrane (SSM)-based electrophysiological experiments (Niessen et al., 2016) using plasma membrane preparations obtained from Torpedo californica. These findings validated and underline
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br Patients and Methods br Results br Discussion
2024-06-25

Patients and Methods Results Discussion Gjerdrum et al showed that Axl Cetrorelix is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cells. Mackiewicz et al also showed that
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Because of the formation of phosphoenzyme
2024-06-25

Because of the formation of phosphoenzyme intermediates, the enzymatic Clofibric Acid of P-ATPases can be divided into steps that include a kinase activity, by which an aspartate residue on the enzyme is phosphorylated, and a phosphatase activity, by which the phosphoenzyme is dephosphorylated. Ano
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