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GSIs were shown to effectively decrease
2021-10-21

GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel
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DMOG br Acknowledgements br Introduction Galanin shows wides
2021-10-21

Acknowledgements Introduction Galanin shows widespread distribution in the central nervous system (CNS) and peripheral nervous system (PNS) as well as in the immune, endocrine and endothelial vascular systems (Lang et al., 2007). Galanin controls diverse physiological processes such as arousal
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miRNAs post transcriptionally regulate gene expression by cl
2021-10-21

miRNAs post-transcriptionally regulate gene brucine by cleaving mRNA or inhibiting translation of target gene transcripts. Vita analysis of HBV genome sequence suggested that miR-185-5p may not directly act on HBV mRNAs, which suggested that miR-185-5p might suppress HBV gene expression and replica
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Cysteine Cys residues are frequently found to
2021-10-21

Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri
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Acknowledgments br INTRODUCTION AND OBJECTIVES br
2021-10-20

Acknowledgments INTRODUCTION AND OBJECTIVES METHODS RESULTS CONCLUSIONS Introduction Class 3 alcohol dehydrogenase (EC 1.1.1.1), also known as ADH5 chi polypeptide in humans, was first identified by Koivusalo et al. [1] as a NAD+-dependent hydroxymethylglutathione (HMGSH) oxidase. By
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To characterize the basic functions of GPR
2021-10-20

To characterize the basic functions of GPR84 in phagocytes, we have utilized the receptor selective antagonist GLPG1205 (a small selective antagonist of GPR84 developed by Galapagos NV [14]) together with ZQ16 (2-(hexylthio) pyrimidine-4,6-diol), a potent GPR84 selective agonist identified in a high
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To combat the detrimental effects of neuropathological
2021-10-20

To combat the detrimental effects of neuropathological conditions, additional therapeutic interventions that either dampen chronic neuroinflammation or attenuate reductions in hippocampal neurogenesis are critically needed. The cannabinoid system has already been shown to rescue impaired neurogenesi
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To gain insights for further improvement of
2021-10-20

To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocycli
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Patient characteristics are presented in Serum
2021-10-20

Patient characteristics are presented in . Serum oestradiol levels on the day of oocyte retrieval or warming were higher in group A (253.2 pg/ml) compared with group B (192.6 pg/ml), despite a significantly reduced number of days (mean 3.5 days) taking oestrogens without the addition of progesterone
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With the nitrogen containing heterocycle components and
2021-10-20

With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic nox4 (, and ), followed by deprotection by TFA, smoothly provided the corr
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Interestingly the subcellular localization of
2021-10-20

Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule ASP015K reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the ability
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Several classes of small molecules
2021-10-20

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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Furthermore a direct thiol protective
2021-10-20

Furthermore, a direct thiol protective role of S-nitrosylation has been reported in animals [66]. Here, formation of higher order irreversible oxidative modifications, such as sulfinic and sulfonic acids were prevented by S-nitrosylation. All these observations underline the important role of ROS in
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One important aspect about GSK
2021-10-20

One important aspect about GSK-3 inhibitors is their effect on pluripotency of MMP-2/MMP-9 Inhibitor I synthesis [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This com
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br Declaration of interest br Acknowledgments br This work
2021-10-20

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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