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br Acknowledgements The authors would like
2023-05-24
Acknowledgements The authors would like to thank Dr. Bradford B. Lowell for providing us with β-less and WT breeding pairs. Funding sources: This work was supported by NIH Grant DK028082 (to E.M.F) and by an Institutional Research Training Grant NRSA 5T32DK751627 (to N.D.). Introduction The e
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A high throughput small molecule ACK biochemical inhibition
2023-05-24
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found glut1 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perfor
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Our co IP data show that HT A or HT
2023-05-24
Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun
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We demonstrate a role for low oxygen
2023-05-24
We demonstrate a role for low oxygen to regulate ATX mRNA in hepatocyte-derived HuH7 Free Fatty Acid Quantification Colorimetric/Fluorometric Kit and human liver slices, consistent with reports of increased ATX expression in a variety of tumours that are frequently hypoxic. Importantly, we show a po
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Pyrimidine is the important pharmacology core in many
2023-05-24
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Valproic acid sodium sa
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isrib synthesis The amino hydroxy methyl isoxazolepropionic
2023-05-24
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic isrib synthesis (AMPA) receptor is also enriched in postsynaptic striatal neurons (Bernard et al., 1997, Kondo et al., 2000, Reimers et al., 2011). Its activity is subjected to the regulation by a mechanism involving phosphorylation (Lu and Roche,
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Torcetrapib We demonstrated clearly that the overexpression
2023-05-24
We demonstrated clearly that the overexpression of sFlt-1 significantly increased arginase Torcetrapib and enhanced arginase activity in HUVECs (Fig. 3). NO formation is related inversely to serum levels of sFlt-1 in preeclampsia [11]. The disorder of NO formation, which was involved in hypertensio
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The crucial role of AP in
2023-05-23
The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch
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Using the same techniques we found that UCP also has
2023-05-23
Using the same techniques, we found that UCP3 also has a half-life of between 1 and 4h [117]. In NHS-12-Biotin to UCP2 and UCP3, UCP1 and ANT had much longer half-lives and could not be degraded in the cell-free reconstituted system, suggesting their degradation is not mediated by the cytosolic pro
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br Concluding Remarks and Future Perspectives
2023-05-20
Concluding Remarks and Future Perspectives Herein, we have highlighted our current understanding of the role of the LKB1-AMPK pathway and its related kinases in β cell biology. β cell-specific genetic models have been particularly useful in delineating precise roles for individual family members
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N-acetyl D-galactosamine Fig shows a possible scheme of
2023-05-19
Fig. 8 shows a possible scheme of the generation of AP(+)-exosomes based on this study. In response to inflammatory stimuli, ERAP1 is secreted from ER into the extracellular milieu through the conventional secretion pathway. On the other hand, exosomes are derived from the endosomal pathway, and are
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Young et al described the role of adenine
2023-05-17
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Adenosine A A agonists have been shown
2023-05-17
Adenosine A2A agonists have been shown to significantly reduce albuminuria in diabetic mice as well as plasma creatinine [24]. Proteinuria was greater in diabetic A2A knock-out (KO) mice than diabetic wild type (WT) mice [24]. Consistent with these findings, our laboratory initially found that prote
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Compound mg was purified as an amorphous colourless powder M
2023-05-17
Compound 3 (29 mg) was purified as an amorphous, colourless powder. Molecular formula C20H28O4 was established by HRESIMS (Fig. S11) and corroborated with 1H and 13C NMR spectroscopic data (Table 1). IR spectrum showed bands for hydroxyl (3433 cm−1) and carbonyl (1686 cm−1) groups. 13C NMR spectrum
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The first natural product described as LO
2023-05-17
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic protein kinase inhibitor from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long time b
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