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br Materials and methods br Results br Discussion Our
2022-06-23

Materials and methods Results Discussion Our liver-specific Gck (−/−) mice and another line of liver-specific mice [13] exhibited impaired glucose tolerance. Furthermore, both knockout mice showed decreased hepatic glycogen content and reduced Pklr and Fas gene Aldicarb in the liver [11]. H
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br Acknowledgments This work was supported
2022-06-23

Acknowledgments This work was supported by a grant CIHR-NSFC China-Canada Joint Health Research from the National Science Foundation of China (Grant Number 81061120525) and the Canadian Institutes for Health Research (Grant number CCI-109605). The authors thank two anonymous reviewers for helpfu
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Recently unimolecular multi functional peptides that combine
2022-06-22

Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with 9-amino Camptothecin and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control
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The active site of PS is located at
2022-06-22

The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed
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Mevastatin br FXR FGF in the control of BAs
2022-06-22

FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, Mevastatin and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synthes
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Receptor interactions and binding mode of in hGPR
2022-06-22

Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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br Other strategies for ferroptosis
2022-06-22

Other strategies for ferroptosis In addition to ROS-generating and GPX4 inactivating nanomaterials, small molecules and genetic manipulation targeting key factors in the ferroptosis pathway have also been tested for their anticancer effects [39,47,48]. Among a myriad of proteins involved in ferro
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In human cancers it has
2022-06-22

In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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The IN gene of the HIV isolate
2022-06-22

The IN gene of the HIV isolate from Papua (CRF01_AE isolate) contains genetic polymorphisms (Fig. 1A) that encode for variant amino acids in the IN protein, based on the Stanford HIVdb mutation interpretation database (Fig. 1B). These variations slightly changed the three-dimensional structure of IN
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Thus regardless of its specific function PTC is associated w
2022-06-22

Thus, regardless of its specific function, PTC52 is associated with plastid activity. During arbuscular mycorrhizal symbiosis, elongated plastids, which are interconnected through thin, tubular plastid projections called stromules, proliferate in arbuscule-containing root cortex cells (Fester et al.
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As part of our discovery efforts searching for small molecul
2022-06-21

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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G protein coupled receptor GPCR ligands can be
2022-06-21

G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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The action of niacin in upregulating cAMP is most likely
2022-06-21

The action of niacin in upregulating cAMP is most likely determined by the milieu of adenylyl cyclase isoforms expressed in macrophages that are responsive to GPR109A activation. Several adenylyl cyclase isoforms, namely AC2, AC4 and AC7, are responsive to the stimulatory action of Gβγ G-protein sub
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br Results and discussion br Conclusion In this
2022-06-21

Results and discussion Conclusion In this study the first binding assays based on a nonlabelled reporter ligand addressing GlyT1 are described. Following the concept of MS Binding Assays recently introduced in our group, binding of the well-known GlyT1 inhibitor Org24598 employed as reporter l
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Elimination of the Q R bridge significantly affected the pro
2022-06-21

Elimination of the Q234–R244 bridge significantly affected the protein pilocarpine hcl but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially retained the bound
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