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br Acknowledgements We thank Dr James Ritchie and his
2021-07-15

Acknowledgements We thank Dr. James Ritchie and his dedicated staff (Deptartment of Pathology, Emory University) for performing measures of serum VPA levels; Sumitomo Pharmaceuticals (Osaka, Japan) for the generous donation of DOPS, which is required for breeding Dbh −/− mice; Pfizer (Sandwich, K
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comt inhibitors br Introduction Identification and correct s
2021-07-15

Introduction Identification and correct storage of seminal stains are crucial for the investigation of sexual assault cases. Actually, undetected ‘cold’ cases involving sexual assault can be solved decades after investigations analysing DNA from stored evidences [1]. Recently, STR analysis and th
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Inhibition of DHODH is reflected by
2021-07-15

Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear Go 6983 (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few selected compounds
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br Electron transfer pathway Intramolecular
2021-07-15

Electron transfer pathway Intramolecular (or inter-domain) electron transfer (IET) in CDH has been studied in much depth [], and similar IET occurs in CcPDH, from the PQQ cofactor in the AA12 domain to the heme b in the AA8 domain. When two kinds of electron acceptors are used for measuring enzym
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Alvocidib flavopiridol is a piperidine chromenone http
2021-07-14

Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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br Results and discussion Compounds were
2021-07-14

Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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Compound A and Compound B Fig were
2021-07-14

Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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The enzyme cyclooxygenase COX or prostaglandin endoperoxide
2021-07-14

The enzyme cyclooxygenase (COX) or prostaglandin endoperoxide H synthase (PGHS) is the key enzyme in the conversion of arachidonic OICR-9429 (AA) into prostaglandins (PGs) [1]. In 1991, researchers found that there were two isoforms of this enzyme called COX-1 and COX-2 with independent genes and d
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Interestingly increased level of both circulating ET
2021-07-14

Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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Thus based on our prior
2021-07-14

Thus, based on our prior results above, we hypothesized that B cells derived from ESCs are also B-1 cells and HSC independent. To test this hypothesis, we induced mouse ESCs on OP9 stromal cells into B-progenitors and transplanted them into sublethally irradiated NOD/SCID/Il2rγcnull (NSG) neonates.
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To develop novel EPAC inhibitors Zhou and co workers optimiz
2021-07-14

To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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EP receptor is known to mediate the protective effect of
2021-07-14

EP4 receptor is known to mediate the protective effect of PGE2 on the respiratory, gastrointestinal and glomerular epithelial lining (Aoudjit et al, 2006, Kabashima et al, 2002, Schmidt et al, 2011). In this study, the expression of asEP4 in the gills was limited to the epithelial lining suggesting
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In vasculature NADPH oxidases NOXs are the
2021-07-14

In vasculature, NADPH oxidases (NOXs) are the main sources of O2− generation that involve in the transfer of electrons to molecular oxygen. Endothelin-1 [25] and thromboxane A2 [26] were reported to induce eNOS uncoupling via upregulation of NOXs. Additionally, inhibition of p47 phox, a subunit of N
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Moving forward the new mathematical model opens doors
2021-07-14

Moving forward, the new mathematical model opens doors for understanding the SCF network, where activity of a component is blunted through mutation or altered in expression in diseased states, and during therapeutic intervention. Computational modeling could reveal underappreciated secondary or tert
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Main Text Post translational modifications by ubiquitin Ub a
2021-07-14

Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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