• Based on the previous report that FXR regulated

  2022-09-21

  

  Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regula

• In summary the SAR of

  2022-09-21

  

  In summary, the SAR of a series of phenylpropanoic acid-free fatty carbenoxolone receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust eff

• GSK1324726A Neither E nor Z FPP synthase catalyzed the react

  2022-09-21

  

  Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase

• br Author contributions br Acknowledgements

  2022-09-20

  

  Author contributions Acknowledgements The work was supported in part by Natural Science Foundation of China (31601995, 31501028) and an internal research grant of Jianghan University (14042). The authors thank HY of Jingchu University of technology for revising the manuscript. Introduction

• br Materials and methods br Results br Discussion

  2022-09-20

  

  Materials and methods Results Discussion It was previously shown that heterologous DNA vaccines composed of fused cDNA fragments encoding chimeric NH2-terminal human HER2 and COOH-terminal rat neu sequences stimulated stronger antibody responses and protective antitumor immunity than either

• On the other hand after injury of the adult

  2022-09-20

  

  On the other hand, after injury of the adult heart, inflammatory monocytes are abundantly recruited to damaged myocardium and they differentiate into monocyte-derived macrophages (MDMs). They have strong proinflammatory phenotype and very limited capacity to promote angiogenesis and cardiomyocyte pr

• NHS Biotin br Materials and methods br Results br

  2022-09-20

  

  Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic NHS Biotin is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate cancer. Howeve

• br Introduction Atherosclerosis is a chronic inflammatory di

  2022-09-20

  

  Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino Ponceau S Staining Solution australia derivative derived from the metabolism of dietary methionine. Epidemiolo

• br Expression profile of GPR

  2022-09-20

  

  Expression profile of GPR35 As noted above, initial studies indicated expression of GPR35 in rat intestine [1] and stomach [2]. Subsequent studies have confirmed significant expression levels in the small intestine, colon and stomach, and this might be relevant in the association between a GPR35

• br TGR Agonists br FXR TGR Dual Agonists In a

  2022-09-20

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• br FXR Agonists Azepinol b indole hEC

  2022-09-20

  

  FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in

• br FXR Agonists Azepinol b indole hEC

  2022-09-20

  

  FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in

• The CO chemosensitivity of the LH PFA has been shown

  2022-09-19

  

  The CO2 chemosensitivity of the LH/PFA has been shown to be dependent on sleep-wake states (B.S. Deng et al., 2007; Dias et al., 2010, 2009; Li et al., 2013). In this context, it was demonstrated that focal acidification of the LH/PFA, by microdialysis of acidic artificial cerebrospinal fluid (aCSF)

• Although it is mainly a glial protein

  2022-09-19

  

  Although it is mainly a glial protein, 5–10% of total GLT-1 represents a neuronal form located at presynaptic terminals, but its physiological role remains elusive (for discussion, see (Rimmele and Rosenberg, 2016)). Nevertheless, this amount might be significant since GLT-1 has been estimated to be

• Nuclear export of GK has been reported to

  2022-09-17

  

  Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros

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