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br Preclinical development of GIP agonists Since the action
2022-04-12

Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a
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Similarly spectrophotometric titrations were carried out und
2022-04-12

Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant 891 band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromic shift of the a
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Knock out mice of FXR showed enhancing cholesterol metabolis
2022-04-12

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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FPR ligands comprise structurally very
2022-04-12

FPR ligands comprise structurally very diverse Methylprednisolone of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones,
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If the manager channel dominates we expect the
2022-04-11

If the manager channel dominates, we expect the increase in debt maturity of treated firms relative to control firms to be more evident in firms with weaker corporate governance where managers are less monitored and have more discretion in changing firm risks. We use the governance index (GINDEX) co
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Recently considerable effort has been invested
2022-04-11

Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most w
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During the activation of the coagulation
2022-04-11

During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium dpat receptor on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit
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br Nanoscale Cortical Actin Remodeling in
2022-04-11

Nanoscale Cortical Actin Remodeling in Regulated Exocytosis The network of cortical Aurora Kinase Inhibitor III is formed by numerous fine actin filaments, which are only about 10nm in diameter [52]. Although the microscale role of the cortical actin network in vesicle exocytosis is well establi
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A more quantitative view of kinase specificity suggests a
2022-04-11

A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing o
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Previous reports have implicated the
2022-04-11

Previous reports have implicated the guanylin/GC-C signalling system as being important in osmoregulation in fish, especially in euryhaline species such as the eel which migrate between freshwater (FW) and seawater (SW) environments at different stages of their life cycle (Comrie et al., 2001a, Comr
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br Conclusion and future perspectives The nicotinic acid rec
2022-04-11

Conclusion and future perspectives The nicotinic cki sale receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid and
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There is no doubt that GPR is a
2022-04-11

There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago
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The GPR gene was included
2022-04-11

The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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The top concern for the clinical use
2022-04-11

The top concern for the clinical use of CRISPR-Cas9 technology is safety. Off-target alterations must be avoided to ensure genome integrity and proper cellular function. WGS found no off-target effects among the top 49 predicted off-target sites. WGS did find 4,658 indels and 1,891 SNVs in sgRNA1/2-
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A further generally applicable approach for
2022-04-11

A further generally applicable approach for the synthesis of N-linked glycopeptides involves the convergent Lansbury aspartylation of glycosylamines. Here, the detrimental formation of aspartimides during the activation of the side chain aspartate can be prevented through the use of Ser/Thr pseudopr
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