• Typically upon chronic agonist exposure GPCRs undergo

  2022-06-13

  

  Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have

• metabolic enzymes For a long time the mechanism for the

  2022-06-13

  

  For a long time, the mechanism for the TG-lowering effect of nicotinic metabolic enzymes has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested the i

• br TGR Agonists br FXR TGR Dual Agonists In

  2022-06-13

  

  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

• Thermal analysis of the NQ peptide was performed with

  2022-06-13

  

  Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different Cytidine 5-triphosphate synthesis levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a

• Even though for almost years GnRH was considered

  2022-06-13

  

  Even though for almost 30 years GnRH was considered the main neuropeptide regulating gonadotropin release in vertebrates, Tsutsui et al. (2000) discovered, in the Japanese quail, Coturnix japonica, a hypothalamic neuropeptide that directly inhibits gonadotropin release, and thus named as gonadotropi

• br Flavonoid function Antioxidants are compounds when presen

  2022-06-13

  

  Flavonoid function Antioxidants are compounds - when present at a lower concentration compared oxidizable substrate - that delay or prevent oxidation of the substrate [14], [106]. Antioxidants act as nucleophiles to reduce an oxidative molecule to prevent its interaction with another molecule [14

• An increased sympathetic tone and the hormone glucagon are t

  2022-06-13

  

  An increased sympathetic tone and the hormone glucagon are the main glucose mobilizing factors [28], [29]. Single-cell transcriptome analysis of human islet cells suggests the expression of Ffar1 not only in β-cells but also in α-cells [30]. Moreover, analysis of rat α-cells indicates that FFAR1 exp

• Furthermore we argued that an inability to encode or

  2022-06-13

  

  Furthermore, we argued that an inability to encode or monitor the temporal sequence of events or episodes in order to discriminate between other similar or related events (encoding what-happened-when) could result in an increased susceptibility to proactive interference and, thus, in principle expla

• br Spatial working memory is GluR A dependent The radial

  2022-06-13

  

  Spatial working memory is GluR-A-dependent The radial maze task also allowed us to study hippocampus-dependent spatial working memory. On spatial working memory tasks, the correct spatial response that the animal must make varies from trial to trial and is dependent on some conditional, trial-spe

• The elective controlled fasting study

  2022-06-13

  

  The elective controlled fasting study in our patient provides further metabolic profiling in patients with GCGR defect. Despite her lean body mass with low weight, at the age of 7 years old she demonstrated a good tolerance for fasting with hypoglycemia APETx2 level, insulin, and counter-regulatory

• br Conclusion br Conflict of Interest

  2022-06-13

  

  Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant

• Cx mimetic peptides short synthetic peptides corresponding t

  2022-06-10

  

  Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino Motolimod sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concentr

• We hypothesize that HBO increases GABA

  2022-06-10

  

  We hypothesize that HBO2 increases GABA activity at the GABAA receptor via a nitric oxide dependent mechanism. Blotting for the phosphorylated β3 subunit of the GABAA receptor should theoretically be increased when there is more GABA activity at the receptor (McDonald et al., 1998). We expected that

• FXR agonists represent an attractive class

  2022-06-10

  

  FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet

• Recently accumulated evidence has revealed a

  2022-06-10

  

  Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu

15945 records 417/1063 page Previous Next First page 上5页 416417418419420 下5页 Last page