• The optimization of the lead compound was initiated

  2020-12-14

  

  The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic LEE011 synthesis moiety with other functional groups led to loss of functional activity against EP4 rece

• Cyclosporine NEORAL Oral Solution Novartis is an immunosuppr

  2020-12-12

  

  Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na

• br Results and discussion br Conclusion Recent

  2020-12-12

  

  Results and discussion Conclusion Recent studies showed that EGFR signaling is involved in inflammatory response in several inflammatory conditions. The normal inflammatory macrophage UNC0638 show EGFR-dependent production of inflammatory mediators. Nevertheless, the development of EGFR inhibi

• EBI and its ligand s EBI was

  2020-12-12

  

  EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines

• Why then is leading strand DNA synthesis reduced relative to

  2020-12-12

  

  Why then is leading-strand DNA synthesis reduced relative to lagging-strand synthesis in rad53-1 mutant Tubacin under replication stress? To gain insight into this question, we first determined whether the firing of late origins in rad53-1 mutant cells contributes to compromised leading-strand synt

• Structural homology modelling Intensive Phyre modelling

  2020-12-12

  

  Structural homology modelling. Intensive Phyre2 modelling [44] was performed using the primary amino 89 25 sale sequence of A1S_0222 as input to generate an atomistic 3D-homology model of A1S_0222. The fit to the SAXS data of the homology model as well as the fit to the data of the E. coli adenine-N

• br Material and methods br Results br Discussion Ligase

  2020-12-12

  

  Material and methods Results Discussion Ligase IV is essential for the final ligation of DSBs through the NHEJ pathway. Its co-factor, XRCC4, has been shown to be important for increasing its activity and stability. Interaction between these two factors have been mapped to the linker region

• The unique property of mutant IDH in producing an

  2020-12-12

  

  The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pre

• DGK is classified into the type II DGK subfamily As

  2020-12-12

  

  DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a

• Diacylglycerol kinases DGK and are

  2020-12-12

  

  Diacylglycerol kinases (DGK) α and ζ are lipid kinases that limit diacylglycerol (DAG)-dependent activation pathways downstream of the TCR (Merida et al., 2015). Their upregulation in tumor infiltrating lymphocytes (TIL) has been linked to generation of hyporesponsive states that contribute to immun

• br Introduction Malaria remains a serious parasitic disease

  2020-12-12

  

  Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans

• Interestingly genome wide association studies

  2020-12-12

  

  Interestingly, genome-wide association studies have linked the chromosomal region harboring RDHE2 (SDR16C5) and seven other genes to stature and growth in cattle, humans, and pigs [30], [31], [32], [33], [34], [35], [36], [37], and beak deformity in chickens [38]. The most recent study specifically

• The aberrant methylation of genes

  2020-12-12

  

  The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr

• Cyanine 5-dUTP In recent years the use of liquid chromatogra

  2020-12-11

  

  In recent years, the use of liquid chromatography/tandem mass spectrometry (LC–MS/MS) has become a preferred approach to measure drugs and metabolites in biological fluids due to its very high selectivity and sensitivity [17], [18], [19], [20], [21], [22], [23], [25], [30]. The great sensitivity of

• The body wall intestine seminal receptacle and

  2020-12-11

  

  The body wall, intestine, seminal receptacle and seminal vesicle in the adult worms were also isolated and homogenized to make microsomal fractions to investigate the relative expression of CYP1A2, CYP2E1 and CYP3A4 in these different organs. In order to get sufficient mass, about 20 individual adul

14937 records 690/996 page Previous Next First page 上5页 686687688689690 下5页 Last page