• br Funding br Conflict of interest statement

  2022-03-07

  

  Funding Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Recent papers have shown that Interferon-free hepatitis C virus (HCV) therapies with

• Furthermore we observed a striking difference

  2022-03-07

  

  Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic cp-690550 type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of sGC. In combin

• DNA methylation is a kind of epigenetic modifications

  2022-03-07

  

  DNA methylation is a kind of epigenetic modifications that can be described as a heritable alteration in gene expression, without any changes in the DNA sequence. Recent evidences suggest that the regulation of DNA methylation status is a frequent and early event in prostate carcinogenesis. For exam

• Despite the rapid development of synthetic

  2022-03-07

  

  Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t

• It was noted elsewhere that several of the variants

  2022-03-07

  

  It was noted elsewhere that several of the variants (i.e., Indel19 and SNP63) that make up the risk haplotypes had unusually large differences in allele frequencies between Africans and non-Africans, as compared with a set of likely neutral loci (Fullerton et al. 2002). This finding was interpreted

• In order to investigate whether this off

  2022-03-07

  

  In order to investigate whether this off-target activity was related to a particular structural feature of this AICAR or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups, respectiv

• 3065 In summary through medicinal chemistry

  2022-03-07

  

  In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on

• The biological activity at GPR

  2022-03-07

  

  The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu

• Migratory properties of Treg are

  2022-03-07

  

  Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing GKT137831 into the inflamed tissue (in this case pancreatic islets). CXCR3 responds to CXCL9,

• br Acknowledgments br Introduction Postmenopausal osteoporos

  2022-03-04

  

  Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by NPS-2143 deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of p

• br Materials and methods br Results br

  2022-03-04

  

  Materials and methods Results Discussion Employment of GIPR signaling, specifically the direction of this manipulation, as a strategy to improve body weight remains a contentious subject of intense scientific investigation [22], [32], [33]. Despite the physiological benefits of GIP on WZ811

• Recently several dual GLP GIP receptor

  2022-03-04

  

  Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously

• It is important to underline that although ghrelin increases

  2022-03-04

  

  It is important to underline that Mifepristone although ghrelin increases the motivation to eat even in fed state, its effects on food intake and reward are blunted in obese animal models (Zigman et al., 2016). This emphasizes also the interconnection between homeostatic regulation of food intake an

• Primarily because secretase was a therapeutic target in AD a

  2022-03-04

  

  Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in

• WAY-600 synthesis Retinal GAL receptor distribution suggests

  2022-03-04

  

  Retinal GAL receptor distribution suggests an intrinsic neuronal control since retina lacks an autonomic innervation, and a signal modulation seems most likely here, acting via GALR1 while GALR2 and GALR3 seem to play a rather minor role in this signal transduction. While sources acting on these ret

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