• The significance of the difference in the DDR binding

  2020-03-05

  

  The significance of the difference in the DDR2 binding specificity towards fibrillar and non-fibrillar collagens is not understood, but may imply differences in biological responses when chondrocytes bind to different collagens in the growth plate. Investigations by Labrador et al. (2001) have shown

• To elucidate whether the impact

  2020-03-05

  

  To elucidate whether the impact of hypoxia on EGFR expression is cell context specific or culturing density dependent, we chose the following cancer Fmoc-Ala-OMe driven by EGFR and evaluated the EGFR expression after hypoxia treatment at different culturing density: a highly aggressive and poorly d

• Nowadays it is possible to

  2020-03-04

  

  Nowadays it is possible to detect the AChE inhibitors by several methods such as gas chromatography-mass spectrometry [11], ion mobility spectrometry [12] and lab-on-chip devices [13,14]. However, almost all instrumental detection techniques that are able to conclusively determine the presence of th

• NPC L expression is both tissue and species specific Consist

  2020-03-04

  

  NPC1L1 expression is both tissue- and species-specific. Consistent with its function, NPC1L1 is mainly localized to the brush border membrane of enterocytes and the canalicular membrane of hepatocytes. NPC1L1, which is expressed in the liver of humans and rats but not mice, mediates cholesterol ON 1

• The quantification and monitoring of

  2020-03-04

  

  The quantification and monitoring of ChEs enzymatic activities have traditionally been associated to environmental studies in order to diagnose the exposure of non-target organisms to specific anti-cholinesterasic agents (Nunes, 2011). The importance of these enzymes as biomarkers of environmental c

• br Materials and methods br Results and discussion

  2020-03-04

  

  Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan

• The in vitro enantioselective metabolism

  2020-03-04

  

  The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m

• In the context of E ligase drug discovery

  2020-03-04

  

  In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 HAM

• Elevated DPP activity has been strongly associated with diab

  2020-03-04

  

  Elevated DPP-4 activity has been strongly associated with diabetes mellitus, IR (Röhrborn et al., 2015), metabolic syndrome (Lamers et al., 2011) and inflammation (Zhong et al., 2015). However, report has it that GC exposure increases DPP-4activity in thymocyte homogenates (Kraml et al., 2003) but t

• The DNA damage response DDR

  2020-03-04

  

  The DNA damage response (DDR) is a cellular mechanism that protects against DNA damage induced by endogenous and exogenous factors, it includes changes in cellular processes such as VX-689 mg regulation, DNA damage repair, apoptosis and chromatin remodeling. In recent years, the DDR has been recogn

• br Experimental section br Results and discussion

  2020-03-04

  

  Experimental section Results and discussion Conclusions In conclusion, we have presented an autocatalytic recycling amplification electrochemical biosensing platform for simple, rapid and ultrasensitive detection of MTase activity by combining methylation-sensitive restriction endonuclease

• A novel series of DHODH inhibitors was developed

  2020-03-04

  

  A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h

• QSAR based on the D structures of ligands plays an

  2020-03-04

  

  QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3

• The secondary objective of the

  2020-03-04

  

  The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do

• Functional studies revealed that these ESR

  2020-03-04

  

  Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea

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