• Molecular docking study of compound was performed

  2019-11-07

  

  Molecular docking study of b-raf inhibitors was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the c

• Notably we demonstrated that EP EP receptor

  2019-11-07

  

  Notably we demonstrated that EP2/EP4 receptor-coupled activation of the cAMP signaling pathway accounted for both up-regulation of COX-2 and down-regulation of LOX, which is consistent with the roles of the cAMP signaling pathway in regulation of COX-2 and LOX by PGE2 in a number of other tissues or

• br Materials and methods br Results br Discussion

  2019-11-07

  

  Materials and methods Results Discussion Here we show expression of the EP1 receptor in the hippocampus of mice and the functional influence of the EP1 receptor on kainic aurora kinase inhibitor induced seizures. Mice lacking a functional EP1 receptor gene displayed a lower tendency to ente

• br Acknowledgement br Introduction Human dihydroorotate dehy

  2019-11-07

  

  Acknowledgement Introduction Human dihydroorotate dehydrogenase (hDHODH), a flavin-dependent mitochondrial enzyme involved in de novo Telatinib biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases such as rheumatoid arthritis and cancer [1], [2], [3]. Leflu

• br Thy nephritis is one of the most

  2019-11-07

  

  Thy1.1 nephritis is one of the most commonly used models to study the course of immunoglobulin A and other mesangioproliferative nephropathies. To date, most of the studies have focused on mesangial and, to a lesser extent, endothelial cell recovery following capillary damage, whereas data concern

• br Methods Ventricular cardiomyocytes from adult male Wistar

  2019-11-07

  

  Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10

• Introduction Obesity constitutes a global healthcare problem

  2019-11-07

  

  Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV

• Hedamycin isolated from Streptomyces griseoruber belongs to

  2019-11-06

  

  Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of Ciclopirox (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)).

• That DGAT mediated hepatic steatosis did

  2019-11-06

  

  That DGAT-mediated hepatic steatosis did not lead to insulin resistance was clearly demonstrated in Liv-DGAT2-low mice by their normal blood glucose and plasma insulin levels, normal glucose and insulin tolerance, normal insulin sensitivity by hyperinsulinemic-euglycemic clamp studies, and normal he

• Defensins are one major class of antimicrobial cationic pept

  2019-11-06

  

  Defensins are one major class of antimicrobial, cationic peptides that are released from 17-Hydroxyprogesterone and imbedded in the mucus layer on mucosal surfaces [45]. They can be categorized into two major families; α- and β-defensins. In humans there are two α-defensin members, defensin 5 (HD5)

• van Linden et al developed a comprehensive

  2019-11-06

  

  van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur

• For most enolases fluoride acts

  2019-11-06

  

  For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby

• Here we describe preparation of three

  2019-11-06

  

  Here, we describe preparation of three stable conjugates that are linked by either oxyester, disulfide, or isopeptide bonds (Fig. 10.1). Each of these conjugates depends upon the prior purification of E2 and ubiquitin proteins that have been engineered to favor specific linkages. For the oxyester- a

• Micafungin In solid tumors such as those in breast

  2019-11-06

  

  In solid tumors, such as those in breast and pancreatic cancer, infiltrating CD68+ or CD163+ tumor-associated macrophages (TAMs) correlate with poor outcome (DeNardo et al., 2011, Kurahara et al., 2011, Shabo et al., 2008). The tumor-promoting function of TAMs is based on their capacity to secrete p

• In the next experiments using a Cell Stress

  2019-11-06

  

  In the next experiments, using a Cell Stress Array kit we assessed the effect of mixture of progestogens on the expression of 26 proteins. One group of proteins including PON3, Phospho-p38a, SIRT2, SOD2, HIF-1 alpha, HIF-2alpha and p27 were upregulated upon progestogen treatment. HIF-1 functions as

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