• All experiments in this study

  2022-02-17

  

  All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human

• Mice with GSTP knock out show

  2022-02-17

  

  Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino N6-Cyclopentyladenosine r

• As disclosed in our preceding paper medicinal

  2022-02-17

  

  As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Erastin lacks an e

• Conjugated BAs via S PR also activate ERK and

  2022-02-17

  

  Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of

• The mD gene obtained from Dr Dimiter S Dimitrov

  2022-02-17

  

  The mD1.2 gene obtained from Dr. Dimiter S. Dimitrov was inserted into a pComb3X vector. The transcription and translation of pComb3X plasmid in cells is inhibited by rifampicin, which binds to bacterial DNA-dependent RNA polymerase. However, in the strain BL21 (DE3) expression system, there is over

• The need for an inflammatory

  2022-02-17

  

  The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab

• In conclusion we have designed and characterized a novel ser

  2022-02-17

  

  In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,

• br Glucocorticosteroid receptor structure and function

  2022-02-17

  

  Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,

• br Phylogenetic analysis of vertebrate receptors for peptide

  2022-02-17

  

  Phylogenetic analysis of vertebrate receptors for peptides similar to glucagon Genes for receptors for peptides similar to glucagon and other secretin-like hormones have been identified in a number of vertebrate species (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et

• Whereas accurate measurement of glucagon in humans has been

  2022-02-17

  

  Whereas accurate measurement of glucagon in humans has been possible since the early 1950s proper measurements in rodents, have not. That said, plasma concentrations of glucagon have been reported in rodent studies [21] using C-terminal specific methods but what has been lacking is the secretory dyn

• While CART increased circulating levels of GIP and

  2022-02-17

  

  While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to

• Although NCT undergoes complex glycosylation processing for

  2022-02-17

  

  Although NCT undergoes complex glycosylation processing for maturation through trafficking from endoplasmic reticulum to Golgi or additional compartments, the effect of NCT glycosylation on γ-secretase activity and substrate specificity is still unknown. The present study focused on glycosylation st

• Determination of enzyme activity differs from other analytic

  2022-02-17

  

  Determination of enzyme activity differs from other analytical procedures. In this gamma-Glu-Cys case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic re

• Another lever to efficiently eradicate tumors including

  2022-02-16

  

  Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing

• According to previous methods several mobile phase compositi

  2022-02-16

  

  According to previous methods, several mobile phase compositions and gradient programmes were assayed to get the best resolved peaks for HA and MHA [12], [13], [24]. Considering the slightly structural differences of the analytes, a mobile phase consisting in two eluents of different polarity and pH

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