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In order to study the
2021-12-16

In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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Compounds and were tested for pharmacodynamic effects in a
2021-12-16

Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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Some years ago it has been described
2021-12-16

Some years ago, it has been described that CD45RA+ CD62L+ naïve CD4+ T letrozole cost can be further differentiated into two distinct subpopulations by analysing their surface expression of CD31(Kimmig et al., 2002a; Kohler and Thiel, 2009; Kohler et al., 2005b). CD31+ thymicnaive CD4+ T cells are
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br Introduction The third variable V
2021-12-16

Introduction The third variable (V3) loop of the gp120 envelope glycoprotein (Env) on the surface of human immunodeficiency virus type 1 (HIV-1) becomes exposed after the virus binds CD4, the initial receptor; the V3 loop plays an important role in contacting the coreceptor CCR5 or CXCR4 to media
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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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