• br Introduction Estrogens play an important role

  2021-06-09

  

  Introduction Estrogens play an important role in the fura 2 am receptor (Arevalo et al., 2015). During several decades, estrogen withdrawal in women has been associated with cognitive impairment, increased Alzheimer's disease (AD) risk (Pike, 2017) and with psychiatric disorders such as schizophr

• br Enzyme activations Activated proteinases

  2021-06-09

  

  Enzyme activations Activated proteinases can unleash a deluge of tissue damage (Zucker et al., 2009). Once activated, the essential enzymes such as serine proteases and cysteine proteases cannot discriminate between self and non-self, burning away self-tissues (Chien et al., 2009, Laskar et al.,

• The elastase induced injury model

  2021-06-09

  

  The elastase-induced injury model has been shown to produce airspace enlargement, and increases in lung volume and compliance that are similar to those observed in human patients (Hantos et al., 2008, Hamakawa et al., 2011). Thus, this model, which has been used to study emphysema, should be adequat

• In the past few years neuroprotection

  2021-06-08

  

  In the past few years, neuroprotection via GLP-1R activation has been shown in several animal models of stroke, Alzheimer's, Parkinson's, Huntington's, ALS and traumatic GNE-617 injury. This research field is rapidly growing and several reviews have been recently published (Darsalia et al., 2014b,

• 3'-O-(2-nitrobenzyl)-2'-dATP Herein in continuation

  2021-06-08

  

  Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)

• Methylation of histone tails is important in regulating chro

  2021-06-08

  

  Methylation of histone tails is important in regulating 94535 structure and transcription. Methylation occurs at arginine and at mono-, di- or tri-methylated lysine residues. The reversibility of histone methylation was recently revealed by the identification of two histone demethylases, LSD1 and JH

• The collagen binding membrane proteins discoidin

  2021-06-08

  

  The collagen-binding membrane proteins, discoidin domain receptors 1 and 2 (DDR1 and DDR2) belong to the family of receptor tyrosine kinase and are expressed in a variety of mammalian cells.7, 8 These transmembrane glycoproteins (∼125 kDa) have been found to be over-expressed or atypically expressed

• brompheniramine maleate It is well established that

  2021-06-08

  

  It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed

• An even more striking difference is observed when comparing

  2021-06-08

  

  An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D9

• br Fragment based drug discovery FBDD is a powerful method

  2021-06-08

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical Aprepitant receptor space with libraries which are smaller in size, producing drug leads with high ligand-binding effici

• br Conflict of interest br

  2021-06-08

  

  Conflict of interest Acknowledgements This work was supported by the Biotechnology Research Center, China Three Gorges University, Yichang, China (No. 2016KBC05), the National Natural Science Foundation of China (No. 31370600 and 31300508), the Zhejiang Science and Technology Major Program on

• br Results and discussion br Conclusions

  2021-06-08

  

  Results and discussion Conclusions An optimization study of the dipeptidyl enoates was performed by chemical structure modifications (Fig. 5). Compound FGA50 displaying R configuration at C-3 was more active than its epimer FGA40. Two modifications of the chemical structure of FGA50 were done:

• racecadotril australia In the livers mefenamic acid ibuprofe

  2021-06-08

  

  In the livers, mefenamic acid, ibuprofen, and meloxicam significantly reduced expression of both 20-HETE and EETs synthesizing cyp450 genes (ANOVA, p value 0.05, Fig. 6). Control group: The lobular architecture and zonal accentuation in the liver of the control group were well preserved and kept i

• Pyrazolopyrimidines are bioisostere of purine exhibit

  2021-06-08

  

  Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase carboxypeptidase a [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour

• Acidic substituents showed moderate biochemical activity but

  2021-06-08

  

  Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic CAY10603 australia were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their bioc

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