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It appears that not all GPR agonists require
2021-09-11

It appears that not all GPR119 agonists require a high dose to elicit acceptable ALW-II-41-27 control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg si
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In accordance with its similarity
2021-09-11

In accordance with its similarity to classical NLSs, Importin α3 was recently reported as a nuclear transport receptor for Ci (). We therefore superimposed the Gli1 NLS model with the Importin α2 structure (3EFX), which has a structure similar to Drosophila Importin α3 () (Fig. 4.4B). Gli1 NLS fitte
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Although exhibited high inhibitory activity was found to be
2021-09-10

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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In cardiomyocytes mechanical stress builds up
2021-09-10

In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans
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In addition to FAK P MAPK kDa polypeptide
2021-09-10

In addition to FAK, P-38 MAPK (38 kDa polypeptide) serves as cross-talk effector for signal transduction, enabling this factor to play a vital role in numerous biological processes (Cuenda and Rousseau, 2007). Pharmacologically modulation of P-38 has shown to be an effective approach in the orientat
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It is known that microglial function
2021-09-10

It is known that microglial function and morphology are closely related [20], but no studies have addressed whether neuroinflammation induced by alcohol might modify microglial 98 9 mg (i.e. morphology, neuroimmunochemical phenotype) through an eCB-dependent mechanism. Since this alcohol-induced mi
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br The HDC knockout mouse as a
2021-09-10

The HDC knockout mouse as a pathophysiological model of TS The implication of a hypomorphic allele of the Hdc gene as a rare cause of TS (Ercan-Sencicek et al., 2010) created a rare opportunity for the generation of a pathophysiologically grounded model of the disorder. Modeling pathophysiology o
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Probucol Fig C presents the secondary structure
2021-09-10

Fig. 1(C) presents the secondary structure arrangement of the PAS-A and PAS-B domains in both HIF-2α and ARNT. The common scaffold of the PAS domains is a β sheet with numerous flanking α helixes. The PAS-A domains of both HIF-2α and ARNT have A’α, Aβ, Bβ, Cα, Dα, Eα, Fα, Gβ, Hβ, and Iβ from the N t
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On the other hand the
2021-09-10

On the other hand, the single-stranded RNA flavivirus hepatitis C virus (HCV), causes type C hepatitis, which often leads to liver cirrhosis, hepatic failure and hepatocellular carcinoma. Its genome of about 9.6kb encodes the structural proteins C, E1, E2, and the nonstructural proteins NS2, NS3, NS
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hexokinase regulation Acknowledgements We appreciated the co
2021-09-10

Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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Two kind systems are currently available to assess
2021-09-10

Two kind systems are currently available to assess the nutritional status of cancer patients, one is largely based on some subjective parameters, the other is totally based on the objective parameters. For score systems largely based on some subjective parameters, like Nutritional Risk Screening Sco
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For the SAR study human haspin kinase inhibitory activity
2021-09-10

For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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br GC C and cGMP of mice
2021-09-10

GC-C and cGMP: of mice and men As is usually the case for many genes, most of the studies that relate to GC-C have to date been carried out in mouse models, or in cell lines derived from human colorectal cancer tissue. What appeared to be a lacuna was any report of a human disorder that resulted
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Our results show furthermore that
2021-09-10

Our results show furthermore, that higher concentrations of butyric Zileuton additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 expression r
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br Materials and methods br Results
2021-09-10

Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic L-Glutamine is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is unclear. Since the
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