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br Material and methods br Results br
2021-11-24

Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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br Materials and methods br
2021-11-24

Materials and methods Results Discussion In this study, we demonstrated, for the first time, that manipulation of AKR1D1 expression and activity is able to regulate glucocorticoid availability in liver and non-liver cell lines. AKR1D1 over-expression leads to increased glucocorticoid cleara
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br Acknowledgments The authors would like to thank principal
2021-11-24

Acknowledgments The authors would like to thank principal investigator Edward John Pratt, MD (Lilly-NUS Centre for Clinical Pharmacology, Singapore) and study investigator Martha Hernandez-Illas MD (QPS-MRA) along with site staff, and trial participants and their families. We thank Zvonko Milice
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Given the important role of
2021-11-24

Given the important role of Cx43 in maintaining the function of gap junctions, to investigate the effects of stress on Cx43 may be an important step towards understanding the mechanism underlying CUS-induced dysfunction of gap junctions. Corticosterone (CORT), as an important stress hormone, has bee
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br Secretase modulators a loss of pharmacology
2021-11-24

γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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Moreover intestinal chronic inflammation is a
2021-11-24

Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic SR 57227 hydrochl
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insulin receptor br BA induced activation of
2021-11-24

BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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DAMPs are endogenous danger signals that
2021-11-24

DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious ecopipam during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our current data indica
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The F P concentration reported for a resting rabbit
2021-11-24

The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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A great number of proteins entering the nucleus possess a
2021-11-24

A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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242 4 Several classes of small molecule inhibitors of
2021-11-24

Several 242 4 of small-molecule inhibitors of FBPase have been reported. These inhibitors can be structurally classified into two groups; non-phosphorus-based inhibitors and phosphorus-based inhibitors. In the former group, several chemotypes including anilinoquinazoline, indole dicarboxylic acid, p
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The hyperacetylation of histone proteins by HATs is known to
2021-11-24

The hyperacetylation of histone proteins by HATs is known to be associated with gene activation [51]. In particular, p300, which is a transcription factor having HAT activity, links activators to the transcription machinery at promoters [52]. The p300/CBP complex dynamically regulates hundreds of di
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Literature review suggests a strong presence of central hist
2021-11-24

Literature review suggests a strong presence of central histaminergic transmission in the Wortmannin areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in the br
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Corollary and Lemma Finally Corollary and Lemma
2021-11-24

(Corollary 3 and Lemma 9). Finally, Corollary 5 and Lemma 10 show that if then the support of is wide enough and so must contain the points of maximum of the attached. However, the support of is too narrow and so does not contain the points of maximum of the remote. Hence, the remote has at most
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So studies are currently in progress to design drugs which
2021-11-24

So, studies are currently in progress to design drugs which could inhibit the main crosstalk components between interacting key pathways (Fig. 1). Wnt The Wnt family consists of 19 highly conserved glycoproteins serving as ligands which bind to the G-protein coupled 7-pass transmembrane receptor
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