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LY3039478 In agreement with the role of ACLY
2023-03-03

In agreement with the role of ACLY in induced macrophage, we observe a drastically reduction of PGE2 levels when ACLY activity is inhibited. This is possible because PGE2 production requires arachidonic acid, which in turn is synthesized by elongation of dietary linoleic LY3039478 with acetyl-CoA p
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Receptor Subtypes and Their Function Critical Appraisal Larg
2023-03-03

Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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Aminoglutethimide first generation aromatase inhibitor
2023-03-03

Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome
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br Introduction The apelin receptor angiotensin
2023-03-03

Introduction The apelin receptor (angiotensin receptor-like 1, APJ) is a seven transmembrane receptor (7TMR) that belongs to the class A peptidergic G protein-coupled receptors (GPCR) superfamily [1]. The endogenous ligands of APJ are the different isoforms of apelin (namely apelin-13, −17, and −
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Cyclo(RGDyK) br Introduction AMP activated protein kinase
2023-03-02

Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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Here we found that AMPK directly phosphorylates EZH
2023-03-02

Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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br Current therapies for metabolic
2023-03-02

Current therapies for metabolic diseases Inborn errors of metabolism caused by deficiency of particular enzymes due to loss of function mutations or deletions have been treated by decreasing the intake of the enzymatic substrate, supplementation with an essential cofactor or vitamin, increasing m
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Pyrintegrin Control of retinal vascularization during develo
2023-03-02

Control of retinal vascularization during development and OIR likely involves close interactions among endothelial cells, neurons and glial Pyrintegrin (microglial and astrocytes) (see Fig. 2). In particular, the interaction between endothelial tip cells and astrocytes plays a critical role in devel
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In the olfactory bulb expression was especially prominent in
2023-03-02

In the olfactory bulb, expression was especially prominent in the mitral cell layer from embryonic stages to adult tissues (Figs. 1D–G). By E14–E16, Ack1 signal was remarkably intense in the proliferative ventricular zone (Fig. 1D). From E18 to adult, expression was also observed in glomerular and g
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Osteoblasts have been thought to be the
2023-03-02

Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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br Antioxidative stress and anti inflammation Oxidative stre
2023-03-02

Antioxidative stress and anti-inflammation Oxidative stress is a major cause of reduced endothelial NO bioavailability in hypertension, and inflammatory response is thought to play an important role in these processes (Blake and Ridker, 2001, Landmesser et al., 2006). Reactive oxygen species (ROS
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Finasteride has been shown to
2023-03-02

Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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To test the compounds metabolic stability we
2023-03-02

To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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br Material and methods br
2023-03-02

Material and methods Results Discussion The present study demonstrates for the first time that Mino selectively induces apoptosis in Jurkat Dasatinib Monohydrate mg via an H2O2 signaling-dependent mechanism. Structurally, Mino is composed of a C10 and C12 phenol group, C12a hydroxyl group,
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The crucial role of AP
2023-03-01

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 chr
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