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In parallel we were also preparing and evaluating other
2021-12-16

In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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br Declaration of interest br Acknowledgments br This work w
2021-12-16

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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In the present study a significant increase in
2021-12-16

In the present study, a significant increase in liver glut4 mRNA levels as well as an increase in liver glycogen content was observed in the dogfish in response to glucose-loading, although we did not observe any changes in liver glycogen content or glut mRNA levels following insulin administration
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GIPR genes were not found
2021-12-16

GIPR genes were not found in any of the available bird genome as well as the genomes of several species of fish (Tables S3 and S4). The genomic neighborhoods surrounding the GIPR genes in species that have them was generally conserved (see Fig. 8), and like GLP2R, those fish that did have a Gipr gen
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One may carefully evaluate the concept pancreas derived GLP
2021-12-16

One may carefully evaluate the concept ‘pancreas derived GLP-1′ as this may dependent on the specificity of the TL32711 used in immunohistochemistry or radiommunoassays. If either a side-viewing antibody or a C-terminal wrapping antibody raised against GLP-1 is applied one may also identify N-termin
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In order t http www apexbt
2021-12-16

In order to validate the correctness of our interpretation of the gap-FRAP data and the analysis of GJC in astrocytes, we used a mathematical model based on morphological and experimental data. This mathematical model is based on SR101 diffusion in an elementary network. In agreement with the morpho
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Developmental studies have reported that some subunits of
2021-12-16

Developmental studies have reported that some subunits of GABAA receptors like α2 and α3 are predominantly expressed during in-utero development, and then substituted for α1 around birth in the rat hippocampus (Brooks-Kayal et al., 2001; Fritschy et al., 1994; Golshani et al., 1997; Kapur and Macdon
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The occurrence of naturally HCV NS
2021-12-15

The occurrence of naturally HCV NS3 resistance-associated substitutions (RAS) affects virological outcome of DAA-based combination therapies [14], [15], [16], [17], [18], [19]. For the majority of NS3 protease inhibitors the frequency of natural occurrence of single RASs in HCV genotype 1-infected p
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Receptor guanylyl cyclases play essential roles in cardiovas
2021-12-15

Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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As disclosed in our preceding paper medicinal chemistry SAR
2021-12-15

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, pi3k inhibitors la
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To support maximal growth and metabolic function
2021-12-15

To support maximal growth and metabolic function of major organs, glucose and Cyclopamine are essential. We assessed the plasma levels of glucose and amino acids in LBW and NBW piglets at birth and at day 7 postpartum. Blood glucose levels were influenced by birthweight and age. In this study, the
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br Gap junctions hemichannels and connexins Molecular charac
2021-12-15

Gap junctions, hemichannels and connexins: Molecular characteristics and function Cell-to-cell communication is of extreme importance in tissue homeostasis, which is maintained by transmission of regulatory signals (Fig. 1). Intercellular communication via gap junctions (GJs) represents one of th
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Our previous study provided some evidence that
2021-12-14

Our previous study provided some evidence that the pre-treatment of livers with rapamycin induces the expression of HO-1 and Prx-1 (Kist et al., 2012). The present results define the dose-response curve for the induction of HO-1 and Prx-1 expression by rapamycin in normal hepatocytes. While, in the
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Senegenin br Introduction Sister chromatid cohesion is estab
2021-12-14

Introduction Sister-chromatid cohesion is established during DNA replication by a ring-shaped cohesin complex consisting of the core subunits Smc1, Smc3, Scc1, and SA1 or SA2, which recruit regulatory subunits Pds5 (Pds5A/B in vertebrates), Wapl, and Sororin to regulate the association of cohesin
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In order to elucidate the mechanisms behind the
2021-12-14

In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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