• Arena Pharmaceutical introduced a biaryl sulfone

  2022-04-13

  

  Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura

• In hypoxic breast cancer cells

  2022-04-13

  

  In hypoxic breast cancer cells, BNIP3-mediated autophagy activation and elevation of amino Antagonist G levels were notable. BNIP3, a BCL-2 family protein, is known to be transcriptionally regulated by HIF-1α and to be involved in cancer cell death in hypoxic conditions [51]. As a link to autophagy

• All the compounds and were assayed for their potential

  2022-04-13

  

  All the compounds –, , , –, , – and – were assayed for their potential cytotoxicity at a single dose of 10 µM on Huh7 cells. Interestingly, all compounds proved to be non toxic, with the exception of and which exhibited high cellular toxicity and therefore were excluded from further experiments (a)

• The characterization of Da CTSL

  2022-04-13

  

  The characterization of Da-CTSL1 shows that it preferentially cleaves Z-FR-AFC (Fig. 8), which has a AVE 0991 phenylalanine at P2 and Da-proCTSL1 is autocatalyzed at pH 8.0 releasing an activated Da-CTSL1 that exhibits optimal activity at pH 8 indicating that the enzyme when secreted by the foregut

• Reduction of the hydrolysis of ATP is an

  2022-04-13

  

  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

• With able to modulate inflammation and effect obesity

  2022-04-12

  

  With ω3 able to modulate inflammation and effect obesity-related outcomes, it is of interested that two G-protein coupled receptors (GPCR), GPR120 and GPR40, were recently deorphanized and shown to recognize ω3 acids (docosahexaenoic, C22:6; eicosapentaenoic, C20:4; and α-linolenic, C18:3), as well

• In addition to redox stress nutritional intake plays a

  2022-04-12

  

  In addition to redox stress, nutritional intake plays a key role in modulating energy metabolism. DIO animal models are commonly used to study altered metabolic changes consequential to fat storage within various fat pads. In general, diets containing >40% high-fat lard, milk, and butter promote exc

• MDL 12330A hydrochloride The differential tissue and ligand

  2022-04-12

  

  The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va

• The importance of FXR FGF signaling in BA homeostasis

  2022-04-12

  

  The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P

• Selection of the month br

  2022-04-12

  

  Selection of the month Fibrosis Liver protection device Non-alcoholic steatohepatitis Genetic metabolic liver disease Hepatitis C virus (HCV) infection Hepatitis B virus (HBV) infection Cirrhosis Regeneration Introduction Upon catalysis by hepatic and bacterial enzymes, c

• In this study we find that DH

  2022-04-12

  

  In this study, we find that DH-CBD induces analgesic effects on inflammatory but not acute pain and the Tideglusib level of spinal α1 GlyRs increased after CFA paw injection. These results suggest that GlyR α1 is only involved in chronic pain. A possible explanation is that once the expression of α1

• br Methods br Results and discussion Protein

  2022-04-12

  

  Methods Results and discussion Protein analysis of commonly used cell lines (C6, D54-MG, U87, U251 and STTG1) reveals high 94 8 sale of SXC (Cho and Bannai, 1990, Ye et al., 1999, de Groot et al., 2005, Lyons et al., 2007, Savaskan et al., 2008). Since protein expression can be altered over t

• protein kinase inhibitor br Materials and methods Rat forebr

  2022-04-12

  

  Materials and methods Rat forebrains were obtained from Sprague–Dawley rats at 2, 7, 14, 21, and 30–35 postnatal days and were homogenized in 1:5 volumes (w/v) of 0.32 M sucrose containing 1 mM EGTA, 1 mM EDTA, 1 μg/ml TPCK, 50 μM leupeptin, and 3 μM antipain with 10 strokes in a glass-teflon ho

• In conclusion atorvastatin but not pravastatin impaired gluc

  2022-04-12

  

  In conclusion, atorvastatin but not pravastatin impaired glucose utilization in C2C12 cells and glucose tolerance in HFD mice, which may be partly due to the inhibition of GLUT4 translocation in muscle cells. The decrease in the cholesterol level induced by atorvastatin may partly account for the in

• Here we used chemogenetic modulation

  2022-04-12

  

  Here, we used chemogenetic modulation of MBH GHSR neurons to address the role of the endogenous ghrelin system in the normal, hyperphagic response to a short-term fast. Studies demonstrating the requirement of an intact ghrelin-GHSR system for the rebound food intake following fasting have been inco

16181 records 485/1079 page Previous Next First page 上5页 481482483484485 下5页 Last page