• Introduction of a chloropyridine group

  2022-10-02

  

  Introduction of a chloropyridine group onto the fluoro derivative (→) leads to a similarly potent compound that exhibits a lower /, and as was observed with (), was rapidly cleared. However, the high clearance of () did not prevent the increase in the concentrations of FAAs even as its plasma levels

• Recently results obtained by our group have demonstrated

  2022-10-02

  

  Recently, results obtained by our group have demonstrated that hEECs are able to secrete NPY into the extracellular medium and that this peptide can induce an increase in the [Ca]i of these cells (Jacques et al., 2003b). In light of these results and those obtained in this study, we can speculate th

• Introduction Post translational modifications to the N

  2022-10-02

  

  Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase

• In various models histamine has

  2022-10-02

  

  In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit

• Although HK localizes mainly to either

  2022-10-02

  

  Although HK localizes mainly to either the cytosol or mitochondria [29], [30], [31] and cardioprotection is associated with increased mitochondrial HK binding, some studies have identified a component of HK located in intracellular vesicles within the cardiomyocyte [48], [61], supporting older data

• phenethyl Mapping PPI networks is challenging

  2022-10-01

  

  Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of phenethyl in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their amphiphilic nature. Furth

• 12198 br Endogenous and synthetic ligands of GPR

  2022-10-01

  

  Endogenous and synthetic ligands of GPR55 There are currently limited commercially available synthetic agonists and antagonists that are specific for GPR55. A large number of studies have investigated the pharmacology of GPR55 4, 23, 25, 30, 31, 32, 33, 34, 35, with contradictory findings reporte

• Conformational changes are observed in the

  2022-09-30

  

  Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F

• Hepatic drug metabolizing enzymes and transporters expressio

  2022-09-30

  

  Hepatic drug-metabolizing Miconazole and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes of nuclear recept

• The structure and activity of GLUT has been most

  2022-09-30

  

  The structure and activity of GLUT1 has been most intensively studied in erythrocytes, in which this transporter makes up 10–20% of membrane protein content. Carruthers has shown that, while GLUT1 can exist and transport glucose as monomers, dimers and tetramers, in erythrocytes GLUT1 exists predomi

• A main finding of this study was that the

  2022-09-30

  

  A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that

• L Family Leguminosae widely distributed in tropical and subt

  2022-09-30

  

  L. (Family Leguminosae) widely distributed in tropical and subtropical regions of the world. As a medicinal and edible plant, it is widely used in Asia, especially in China, Korea, Japan and India. It was first recorded in Shen Nong Ben Cao Jing (神农本草经), and was described having the effect of cleari

• br Experimental br Acknowledgments This project

  2022-09-30

  

  Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t

• The widespread involvement of HH GLI in human malignancies

  2022-09-30

  

  The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA

• In Solloway and colleagues reported that mice

  2022-09-30

  

  In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino AS-252424 dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin’ (mT

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