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br Material and methods br Results br
2021-09-16
Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In NNC 55-0396 to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]. This sy
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PBI is an agonist of GPR and acts
2021-09-16
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br Summary br Acknowledgement br
2021-09-16
Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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For many plasma membrane receptors
2021-09-16
For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an
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br Introduction The brain contains
2021-09-15
Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in d
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br Expression and Purification of LSD Proteins
2021-09-15
Expression and Purification of LSD1 Proteins In Vitro Enzymatic Assays Analysis of LSD1 Demethylase Activity Acknowledgments Conflict of Interest Statement: Y.S. is a cofounder of Constellation Pharmaceuticals, Inc. and is a member of its scientific advisory board. Y.S. is also a consu
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br ABT aR aR methyl hexahydropyrrolo b pyrrol
2021-09-15
ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo
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Sometime ago we have described diamino triazines as histamin
2021-09-15
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by L-703,664 succinate and zymosan. In this work we describe
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br Conclusion The hub gene KIBRA
2021-09-15
Conclusion The hub gene KIBRA and the Hippo signaling pathway were downregulated and miR-21 was upregulated in LAD. MiR-21 promoted the viability and mobility of LAD cells, reduced apoptosis and suppressed the Hippo signaling pathway in LAD through targeting KIBRA. Funding The study was appro
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Hippo Signaling in Cancer Immunity The Hippo pathway has evo
2021-09-15
Hippo Signaling in Cancer Immunity The Hippo pathway has evolutionarily conserved roles in limiting the size of organs [1]. It is a kinase cascade regulating transcriptional complexes in response to various upstream signals (Box 1). At the cellular level, the Hippo pathway inhibits cell proliferati
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br Other mechanisms In vitamin B deficiency antibody product
2021-09-15
Other mechanisms In vitamin B6 deficiency, antibody production may be indirectly impaired [38]. Grindley et al. [4] showed that high dietary intake of vitamin B6 (74.3 mg PN/kg diet) suppresses herpes simplex virus type 2 transformed cell-induced tumor growth and enhances immune status compared w
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Our observations with RBC in human platelets suggested a
2021-09-15
Our observations with RBC8 in human platelets suggested a more wide-ranging role for Rals in platelet function compared to our observations in Ral deficient mouse platelets. Using lumi-aggregometry, 10 μM RBC8 significantly reduced platelet aggregation and ATP secretion responses in both WT and DKO
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br Materials and methods br Results As
2021-09-15
Materials and methods Results As expected, due to matching by age, the mean ages were similar for the two groups of children when stratified by ASD status; children with an ASD had a mean age of 67.0 months, while the mean age for children in the TD control group was 68.0 months. Nearly all of
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Our synthetic approach to GPR antagonists was designed so th
2021-09-15
Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic Imiquimod hydrochloride to 4-piperidone by fir
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We first set out to identify the
2021-09-15
We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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