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There were significant differences in mRNA expression
2022-07-29

There were significant differences in mRNA expression levels observed for 7 out of 15 analyzed genes. This observation suggests, that selection of a reference/control group may influence interpretation of gene expression studies performed in liver pathologies. This study directly evidenced that anal
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A number of anti diabetic
2022-07-29

A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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Rare mutations can impair the molecular function of GR and
2022-07-29

Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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Consistent with recent independent studies we confirm that t
2022-07-29

Consistent with recent independent studies, we confirm that the GCG-induced increase in oxygen consumption is only partially blunted in Fgf21−/− mice [32], implicating additional GCGR-dependent mechanisms contributing to the acute GCG-dependent enhancement of energy expenditure. Notably, glucagon ad
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br Conclusion In the present
2022-07-29

Conclusion In the present study, we found that the majority of commercially available antibodies and antibody-based tools against galanin and its receptors that we tested do not meet validation requirements. Therefore, critical validation of these tools by the user is essential before being used
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An advantage of photolabeling with tritiated photoprobes fol
2022-07-29

An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled dna ligase and to quantify photoincorporation which enables assessment of pharmacological specificity and allosteric interactions with other l
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N,N-Dimethylsphingosine The extensive worldwide research eff
2022-07-29

The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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Recent studies have elucidated a profound role
2022-07-29

Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty ro5 or synthetic ligands h
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As a part of our
2022-07-29

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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At the heart of ferroptosis is
2022-07-29

At the heart of ferroptosis is a process of lethal lipid peroxidation, which is the oxidative addition of molecular oxygen (O2) to lipids, such as polyunsaturated fatty acyl tails in phospholipids. The first descriptions of such enzymatic reactions were in 1955 by Peterson and colleagues [50] and Ro
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Several other assay parameters were also explored First
2022-07-29

Several other assay parameters were also explored. First, the thermal dependence of the assay was investigated by measuring the specific activity at different temperatures (Fig. 7). That data show that enzymatic activity increases with increasing temperature. Interestingly, the observed rate increas
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During the activation of the coagulation
2022-07-29

During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium crizotinib on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit pla
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Though studied less extensively than in cholangiopathies
2022-07-28

Though studied less extensively than in cholangiopathies and fatty liver diseases, the Hh pathway is active in other forms of human liver disease, such as Schistosomiasis[58], [101] and chronic viral hepatitis,[100], [125] as well as in several animal models of liver disease, including drug-induced
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biotin-LC-LC-tyramide br Disp Mediated Hh Membrane
2022-07-28

Disp-Mediated Hh Membrane Recycling Due to its cholesterol modification, Drosophila Hh enriches on sphingolipid-rich apical membranes of polarized epithelial biotin-LC-LC-tyramide 33., 38., 39.. Genetic studies examining Hh release from wing imaginal disc epithelia suggest that Hh must be endocyt
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Acknowledgements We appreciated the contributions of
2022-07-28

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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