• The effect of the selected compounds on

  2021-11-12

  

  The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound

• In our reporter assay system

  2021-11-12

  

  In our reporter assay system, C3H10T1/2-Gli1-Luc cells were incubated with Shh CM to induce Gli1-mediated luciferase activity (Fig. 1B). Z-Ajoene inhibited Shh CM-induced luciferase activity in a concentration-dependent manner as seen in Fig. 1C. Z-Ajoene also inhibited SAG (a Smo activator)-induced

• br Some general considerations on anterior pituitary

  2021-11-12

  

  Some general considerations on anterior pituitary cell type, models, sex and drugs Historically, real-time analysis of native endocrine anterior pituitary cell excitability has been somewhat limited and thus much of the pioneering work on anterior pituitary cell excitability and stimulus-secretio

• Experiments show that CSD propagation can be

  2021-11-12

  

  Experiments show that CSD propagation can be slowed or interrupted by pre-existing lesions or areas of high astrocytic density (Chen et al., 2006), and reduced expression of astrocytic gap junctions significantly increases the size of ischemic infarcts (Nakase et al., 2003). By decreasing the gap ju

• When we compared the effects in FST induced

  2021-11-12

  

  When we compared the effects in FST induced by GAL and GAL(1–15), we observed that the increase in the immobility induced by GAL(1–15) was significantly higher than the one induced by GAL (Millon et al., 2015). Moreover, in climbing behaviour, GAL(1–15) also induced a stronger decrease in climbing r

• This review is an overview on

  2021-11-12

  

  This review is an overview on the ongoing trials involving anti-FGF-FGFR therapies (Wu et al., 2013). Pathway FGFR in cancer A recent study comparing more than 4800 tumor tissue samples has shown that 7.1% of all tumor types have genetic alterations in the FGF-FGFR axis. The aberrations perce

• In the previous paper we described the design and

  2021-11-12

  

  In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In

• Genome wide binding and transcriptome analyses demonstrate t

  2021-11-12

  

  Genome-wide binding and transcriptome analyses demonstrate that Fbxl10 directly binds the Areg, Mdk, Lmnb1, Thbs1, Mgp and Cxcl12 locus and thereby might influences the expression of these migration associated genes. The expression of epidermal growth factor (EGF)-like molecule Amphiregulin (Areg)

• Fig illustrates the different signaling pathways elicited or

  2021-11-12

  

  Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime

• Almost all of the series and compounds exhibited

  2021-11-12

  

  Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esteri

• Studies have demonstrated the paradoxical role

  2021-11-12

  

  Studies have demonstrated the paradoxical role of HO-1 in tumorigenesis. At initial stages of carcinogenesis, it protects DNA by lowering the ROS-mediated mutational rate, but later, HO-1 promotes cancer cell survival and proliferation. One PDAC therapeutic strategy is to increase ROS production and

• While phosphorylation site motifs are typically described

  2021-11-12

  

  While Crenolanib site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase,

• Subcellular domains where Rac is

  2021-11-11

  

  Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho

• Importance of glucokinase in glucose homeostasis and a

  2021-11-11

  

  Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl

• Until now various reports have demonstrated the therapeutic

  2021-11-11

  

  Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and

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