• Conjugated BAs via S PR

  2021-12-27

  

  Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of

• The current study also inferred that MT

  2021-12-27

  

  The current study also inferred that MT content in Crassostrea gigas might be associated with the Cd level, and can be affected by MT turnover. The glycosylase of MT in cytosol is beneficial for aquatic organisms to adapt the seawater contaminated by heavy metals, and MT is a biomarker for marine i

• br Acknowledgments This work was

  2021-12-27

  

  Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 81703451) and the China Postdoctoral Science Foundation Grant (No. 2017M611269). Introduction According to the International League Against Epilepsy (ILAE), epilepsy is generally defin

• The SLC A mutations identified in both families

  2021-12-27

  

  The SLC45A1 mutations identified in both families appear to be hypomorphic given that they resulted in a reduction but not abolition of intracellular glucose transport by SLC45A1 in our in vitro assay. It is tempting to speculate that recessive mutations causing a more severe dysfunction of the tran

• Genomic studies have afforded new

  2021-12-27

  

  Genomic studies have afforded new insight into the influence of PI3K Akt mTOR Compound Library structure on GR binding. An important clue came from genome-wide mapping of chromatin structure using DNase I hypersensitive site sequencing (DNase-seq), and comparing the locations of open chromatin to G

• As early as glucagon was shown

  2021-12-27

  

  As early as 1957, glucagon was shown to increase brucine expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27]. This cont

• br Conclusions br Acknowledgement Work in the authors labs

  2021-12-24

  

  Conclusions Acknowledgement Work in the authors’ labs was funded by Natural Sciences and Engineering Research Council of Canada (OGP0194652 and OGP0041653) and Diabète Québec. Introduction Fifty years ago, Sydney Brenner proposed Caenorhabditis elegans as a useful model for the study of an

• The co crystal structure of GPR complexed

  2021-12-24

  

  The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly

• FG2216 Evidence indicates that astrocytes play

  2021-12-24

  

  Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in

• br Retrieval requires histamine H receptors

  2021-12-24

  

  Retrieval requires histamine H1 receptors in dorsal hippocampus Retrieval is a dynamic process that requires neurotransmitter regulation (Barros et al., 2000, Barros et al., 2001). Recently, histamine, and histaminergic transmission has entered the list of putative neurotransmitter modulators of

• br Experimental br Acknowledgements This work was financiall

  2021-12-24

  

  Experimental Acknowledgements This work was financially supported by Ministry of Knowledge and Economy (10032113) and Ministry of Education, Science and Technology (20100000297). Introduction To ensure accurate chromosome segregation, cohesion between sister chromatids must be maintained u

• The hypothesis that genes involved in type diabetes evolved

  2021-12-24

  

  The hypothesis that genes involved in type 2 diabetes evolved under changing selective pressures and may carry the signature of natural selection motivated us to describe patterns of sequence variation at CAPN10 and GPR35 in human populations. An initial population genetics study reported an unusual

• We hypothesized that modulating redox stress

  2021-12-24

  

  We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re

• Because of its excellent GPR potency good hERG selectivity a

  2021-12-24

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, CD 3254 synthesis was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensiv

• In respect of clinical development Takeda has pioneered

  2021-12-24

  

  In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul

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