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The cytotoxicity of these compounds against Hep B
2021-09-14

The cytotoxicity of these compounds against Hep3B cells was assessed using the MTT assay. As shown in , compounds in series and (except ), which retained the carboxyl at C-17, showed no appreciable cytotoxic activity (IC > 100 μM), whereas compounds in series (except ,) were modestly cytotoxic, i
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br Materials and methods br Author contributions br Acknowle
2021-09-14

Materials and methods Author contributions Acknowledgments We thank members of the Skaar laboratory for critical evaluation of the manuscript. This work was supported by grants from the National Institutes of Health, R01AI069233 (EPS), and T32GM008554-21 (LJL). Introduction Pseudomonas
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br Mechanisms of HDAC inhibition
2021-09-14

Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr
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Introduction Post translational modifications to the N termi
2021-09-13

Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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calculate molarity of solution br Acknowledgements br Introd
2021-09-13

Acknowledgements Introduction The glutathione S-transferase (GST, EC 2.5.1.18) family of multifunctional enzymes plays a particularly important role in cellular detoxification [1]. Over-expression of the GSTP1 isoform characterizes many human tumor cell lines derived from stomach, brain and c
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br METHODS br RESULTS br Discussion Numerous studies have pr
2021-09-13

METHODS RESULTS Discussion Numerous studies have proposed various hypotheses and models to explain how neuroinflammation could contribute to the chronic fatigue, postexertional fatigue, and cognitive deficits observed in patients with ME/CFS.12, 13, 14, 15 Although neuroimaging studies have
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IC is a rat mAb specifically binding to insulin granula
2021-09-13

IC2 is a rat mAb specifically binding to insulin granula [127,128]. Although this mAb was discovered 30 years ago, it has only recently been used for β-cell imaging in vivo. Moore et al. used this mAb for β-cell imaging in 2001 [129]. After DTPA conjugation, IC2 was labeled with 111In. Both in vitro
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LPC OMe LPC LPC and OMe LPC were shown
2021-09-13

LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated guanabenz
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br Cell origin The ontogeny of astrocytes in
2021-09-13

Cell origin The ontogeny of astrocytes in vitro has been investigated in detail; Raff et al. (1983) characterised two types of astrocytes: type 1 being fibroblast-like in morphology and poorly labelled with a monoclonal antibody (AB25), whereas type 2 exhibited oligodendrocyte or neuron-like morp
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LbGlcK and the HsHxKIV d glucose complex
2021-09-13

LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key chemokine receptor binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such
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JP 1302 dihydrochloride To synthesize the azaindole based co
2021-09-13

To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic JP 1302 dihydrochloride was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position resulted 3-iodo-7-azaindazole . Alky
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ppar antagonist Previously we have shown that ghrelin and
2021-09-13

Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo
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br Experimental br Results and discussions br
2021-09-13

Experimental Results and discussions Conclusion Notes Introduction The noncanonical DNA structures that is, i-motif [[1], [2], [3], [4], [5], [6], [7], [8], [9]] and G-quadruplex [[10], [11], [12], [13], [14]] have recently been carefully studied using either experimental or computati
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Several observations about structure activity relationships
2021-09-13

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic imidazole sale class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether lin
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Together the epigenetic interplay revealed in this study
2021-09-13

Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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