• The AURA trial was a phase I II study

  2021-01-07

  

  The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,

• In the context of E ligase drug

  2021-01-07

  

  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 L-7

• Similarly synthetic analogs of Alogliptin

  2021-01-07

  

  Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in

• Our observation that FAK is downregulated in vascular

  2021-01-07

  

  Our observation that FAK is downregulated in vascular smooth muscle 516 3 receptor on fibrillar collagen confirms observations reported for other cell types [14]. However, unlike the results reported previously [14], our work suggests that matrix rigidity per se does not determine FAK downregulatio

• Cysteine protease activities have been suggested to be impor

  2021-01-07

  

  Cysteine protease activities have been suggested to be important for Giardia’s pathogenesis [[11], [12], [13],16,18,19,21,28,29,35]. Recently several giardial CPs were shown to be released during host cell interactions [9,10]. The three major released CPs have recently been shown to be involved in t

• It has been reported that CysLT receptors negatively regulat

  2021-01-07

  

  It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge i

• br Materials and methods br Results br Discussion CDK

  2021-01-07

  

  Materials and methods Results Discussion CDK and their regulatory cyclins form a family of heterodimeric kinases that are particularly important for regulation of Aminophylline progression and transcription in tumor cells. These kinases therefore constitute biomarkers of proliferation and

• br Results br Discussion Unraveling the molecular details of

  2021-01-07

  

  Results Discussion Unraveling the molecular details of nucleoporin-karyopherin interactions, which have to be strong enough to promote transport but sufficiently weak to avoid stalling of transport complexes within the pore, is key to our understanding of the mechanisms of nucleocytoplasmic tr

• We showed for the first time that ivermectin significantly r

  2021-01-06

  

  We showed for the first time that ivermectin significantly reduced the pH-induced response of the pHCl-A variant at 300nM, whereas fipronil and γ-BHC had no significant effects on the channel unlike in RDL and GluCl (Fig. 4). Such a concentration is similar to the threshold at which ivermectin activ

• Our previous high throughput screening HTS campaign using

  2021-01-06

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Aminoallyl-dUTP assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22

• Enzyme mimics belong to a type of rising catalysts which

  2021-01-06

  

  Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a

• The activity of cysteine endopeptidases involved in the

  2021-01-06

  

  The activity of cysteine endopeptidases involved in the germination of caryopses is generally regulated at two levels: the hormonal induction of synthesis by gibberellins (Drzymała et al., 2008) and a putative regulation of activity by phytocystatines (Kiyosaki et al., 2007, Martinez et al., 2009),

• The DDRs have also been

  2021-01-06

  

  The DDRs have also been shown to be regulators of certain immunological functions. DDR1 is expressed in stimulated peripheral blood mononuclear pge2 (Kamohara et al., 2001) and on activated T cells (Chetoui et al., 2011, Hachehouche et al., 2010, Kamohara et al., 2001). DDR1 can mediate cell migrat

• In our study the TIP P model is applied for

  2021-01-06

  

  In our study, the TIP3P model is applied for water, AMBER99sb force field [24] is used to describe three types of EGFR, including the wild type (PDB: 2ITY) [25], its mutant G719S (PDB: 2ITO) [25] and mutant T790M (PDB: 3IKA) [26]. The force field of Tubemoside molecule is parameterized with optimize

• EBI and its ligand s

  2021-01-06

  

  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

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