• Two distinct mechanisms have been described for

  2021-09-11

  

  Two distinct mechanisms have been described for niacin’s macrophage-based actions [21,22]. First, niacin blocks recruitment of macrophages to atherosclerotic lesions. Second, niacin upregulates macrophage ABCA1 and ABCG1, transporters involved in reverse cholesterol transport. Upregulation of choles

• br Redox regulation in the brain Reactive oxygen species are

  2021-09-11

  

  Redox regulation in the brain Reactive oxygen species are generated in Eribulin mesylate by the mitochondrial respiratory chain, which occurs on the inner mitochondrial membrane (Murphy, 2009, Jensen, 1966, Dickinson and Chang, 2011). Interestingly, although most cancer cells are thought to prima

• To confirm the in vitro findings

  2021-09-11

  

  To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g

• Prion diseases are transmissible and result in fatal neurode

  2021-09-10

  

  Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in topoisomerase lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can fo

• br Hippo pathway signalling The Hippo pathway is an evolutio

  2021-09-10

  

  Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular Probenecid status [10]. This pathway is linked to development, cell prolifera

• eletriptan Reduction of the hydrolysis of ATP is an importan

  2021-09-10

  

  Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct

• Lipid sensing GPCRs as therapeutic targets G protein

  2021-09-10

  

  Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately

• br Concluding remarks Several orphan GPCRs have expression

  2021-09-10

  

  Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas

• Gene expression of both GPR A and GPR

  2021-09-10

  

  Gene expression of both GPR109A and GPR81 in adipocytes has been linked to PPARγ activation [22]. Treatment with the thiazolidinedione (TZD) PPARγ agonist, rosiglitazone, increases GPR109A and GPR81 expression, and knockdown of PPARγ suppresses receptor expression in fully differentiated human multi

• br Materials and methods br Results shows serum FSH LH

  2021-09-10

  

  Materials and methods Results shows serum FSH, LH, oestradiol and progesterone values in the two cycles from day 2 to day 10. Basal values of these hormones on day 2 (before any intervention) were similar in the two cycles. Thereafter, FSH values did not differ significantly between the two c

• In vitro studies have shown that

  2021-09-09

  

  In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found t

• The molecular identity of RA s target

  2021-09-09

  

  The molecular identity of RA’s target during LTP induction was determined by pharmacological testing. The inhibitory effects of CNQX and niflumic acid on LTP induction remained even in the presence of RA, indicating RA did not affect either the AMPA receptor nor chloride channel (Fig. 2B and D) [26]

• Ethanol decreased the value of desensitization

  2021-09-09

  

  Ethanol decreased the τ-value of desensitization for GluR-Di. Coexpression of stargazin or γ4 further increased the effect of ethanol on desensitization (Fig. 3A, B). The highest ethanol concentration tested (200mM) reduced the τ-value by 16.5±4.9% (n=5) in the control receptors and by 29.3±9.3% (n=

• One effective approach to fine tuning the lipophilicity prof

  2021-09-09

  

  One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic AS-252424 scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as Amge

• All of the abovementioned effects

  2021-09-09

  

  All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra

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