• Various strategies have been pursued in the search for GIPR

  2022-01-19

  

  Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino 2-APB substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g. Pro3(G

• br Gamma secretase trafficking GS activity for APP

  2022-01-19

  

  Gamma-secretase trafficking GS activity for APP can be influenced by sub-cellular trafficking, as APP cleavage differs depending on its localization. APP is synthesized in the ER and transported to the trans-Golgi network (Annaert et al., 1999, Pasternak et al., 2003, Ray et al., 1999a, Rechards

• In recent years many studies have demonstrated

  2022-01-19

  

  In recent years, many studies have demonstrated that the release of endogenous FPR ligands can influence severe diseases associated with inflammation, including systemic inflammatory response syndrome (SIRS)20, 21 and cancers, such as glioblastoma as well as gastric and colorectal cancer 22, 23, 24.

• A species specific diverse number of

  2022-01-19

  

  A species-specific diverse number of FPPS genes are present in insect genomes (Zhang and Li, 2008, Cusson et al., 2006). The genome of the yellow fever mosquito Aedes aegypti contains a single FPPS gene (AaFPPS) that is highly expressed in the CA (Nouzova et al., 2011). FPPS catalytic activity in th

• The membrane metalloendopeptidase MME gene

  2022-01-19

  

  The membrane metalloendopeptidase (MME) gene is located at human chromosome 3q21-27. It encodes a 100-kD type II transmembrane glycoprotein, a widely expressed membrane metalloendopeptidase that degrades a number of substrates. The active site of the enzyme faces the extracellular space. MME is wide

• Contrary to the transient nature

  2022-01-19

  

  Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system

• Here we show in contrast to previous work that

  2022-01-19

  

  Here we show, in contrast to previous work, that several phenotypes associated with Orb6 inactivation, including increased cell width, are independent of Gef1. We further find that Orb6 positively regulates exocytosis, also independently of Gef1. To identify novel targets of Orb6, we performed quant

• The relaxant response to carperitide was influenced

  2022-01-18

  

  The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is e

• Studies dealing with the effects of ischemia on EAATs have

  2022-01-18

  

  Studies dealing with the effects of ischemia on EAATs have been previously reported, but some discrepancies in literature appear between them probably as a consequence of the different models, species, time of reperfusion after ischemia and age of the animals. Thus, in human, Guanfacine hydrochlorid

• br Glucocorticoid receptor and metabolic syndrome GCs acting

  2022-01-18

  

  Glucocorticoid receptor and metabolic syndrome GCs acting through the GR regulate key enzymes of glucose metabolism in the liver, skeletal muscle, adipose tissue and the pancreas. In the liver, GCs regulate the expression of major gluconeogenic enzymes such as phosphoenolpyruvate carboxykinase, g

• In patients with type diabetes glucagon receptor antagonism

  2022-01-18

  

  In patients with type 2 diabetes glucagon receptor antagonism led lowered fasting glucose however not postprandial glucose levels [9], which may reflect that glucagon may not be of particular importance for the diabetic hyperglycemia upon a meal. Current glucagon receptor antagonists have however be

• Recently unimolecular multi functional peptides that combine

  2022-01-18

  

  Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with α-Bungarotoxin receptor and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose cont

• MLN120B Our initial lead optimization started with the modif

  2022-01-18

  

  Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li

• Michiel S van der Heijden had

  2022-01-18

  

  Michiel S. van der Heijden had full access to all 2449 data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven. Wang, Sustic, de

• To meet the requirement of ferroptosis based therapy

  2022-01-18

  

  To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous

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