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In addition to SAHA SBHA also showed a
2021-09-06
In addition to SAHA, SBHA also showed a strong rescue effect. SAHA is a general inhibitor of HDAC function (Finnin et al., 1999, Kim and Bae, 2011), while SBHA is more specific, and has been shown to inhibit HDAC1 and HDAC3 (Richon et al., 1998). The relative level of suppression was similar in Kis
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Several classes of small molecules that modulate CDK activit
2021-09-06
Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati
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Cdc is also linked to the adherens junction via IQGAP
2021-09-06
Cdc42 is also linked to the adherens junction via IQGAP1, however, it appears to have an opposite effect on junctional stability. When Cdc42 is inactive, IQGAP1 binds to β-catenin, displacing α-catenin, resulting in the loss of α-catenin-linked Proteinase K filaments from the adherens junction and
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Type diabetes mellitus T DM
2021-09-06
Type 2 fasudil (T2DM) causes vascular complications and is a major public health problem associated with lifestyle diseases such as obesity, liver steatosis, hypertension, and so on. Although serum lactate is reportedly elevated in diabetic patients [12], [13], the physiological effects remain uncl
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br Materials and methods br
2021-09-06
Materials and methods Results Discussion Conclusion Pharmacophore modeling was applied to explore new probable Glo-I inhibitors. Ninety two pharmacophoric models were generated representing diverse types of interaction between co-crystallized ligands and corresponding binding site. The g
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In order to elucidate the reasons
2021-09-03
In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen YM 022 of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM), while the s
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Two pathways have emerged to
2021-09-03
Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an
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In order to test the
2021-09-03
In order to test the influence of the initial depolarization, experiments were performed, where the degree of chloride substitution was varied, either by adding n-Ringer to Ketorolac tromethamine salt incubated in a sucrose Ringer or by suspending the cells directly in Ringers identical to the fin
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br STAR Methods br Introduction Secretase is a membrane
2021-09-03
STAR★Methods Introduction γ-Secretase is a membrane-embedded proteolytic complex belonging to a diverse family of intramembrane-cleaving proteases and is composed of four integral membrane proteins: presenilin (PS), nicastrin (NCT), anterior pharynx-defective 1 (Aph-1), and presenilin enhancer
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Recently a lot of synthetic
2021-09-03
Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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br Introduction The fibroblast growth factor receptor
2021-09-03
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, amikacin sulfate progression, metabolism, and survival. In non–small-cell lung cancer, the
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Enhancer of Zeste Homolog EZH is
2021-09-03
Enhancer of Zeste Homolog 2 (EZH2) is a core component of the Polycomb Repressive Complex2 (PRC2) which also includes SUZ12 and EED. PRC2 represses gene transcription through trimethylation of Lys27 of histone H3 (H3K27), and contribute to the maintenance of cell identity, Swainsonine australia regu
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In the present study we investigated the
2021-09-03
In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip
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Literature review suggests a strong presence
2021-09-03
Literature review suggests a strong presence of central histaminergic transmission in the rilpivirine areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in the b
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br STAR Methods br Acknowledgments We
2021-09-03
STAR★Methods Acknowledgments We thank P. Adler, V. Riechmann, N. Tapon, E. Knust, the Vienna Drosophila RNAi Center, the Australian Drosophila Research Support Facility (www.ozdros.com), the Bloomington Drosophila Stock Center, and the Developmental Studies Hybridoma Bank for D. melanogaster s
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