• Also a large number of small molecules are

  2021-10-20

  

  Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [

• With the identification of small

  2021-10-20

  

  With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met

• The precise mechanism by which erastin

  2021-10-20

  

  The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A

• Fas ligand FasL the natural

  2021-10-20

  

  Fas ligand (FasL), the natural ligand of Fas, can interact with Fas and thus induce cell apoptosis through the cascade of death signal in various cell types [8]. Additionally, Fas, which is a member of the tumor necrosis factor (TNF) receptor superfamily and death receptor family, is one kind of tra

• A previous study from our institution showed

  2021-10-20

  

  A previous study from our institution showed moderate correlation between the APTT and Anti-FXa assays, prompting an institution-wide change to an Anti-FXa based monitoring of unfractionated heparin. The current study is a descriptive analysis to evaluate the clinical outcomes in this pediatric coho

• Here we showed that microinjection of siRNA

  2021-10-20

  

  Here we showed that microinjection of siRNA at the MII stage efficiently reduced endogenous EZH2 mRNA and protein. Although the percentage of cleaving embryos was not affected, Kaempferol-3-rutinoside formation and blastocyst cell number were both reduced in EZH2 knockdown groups (Table 1). Similar

• br Materials and methods br Results br Discussion The major

  2021-10-20

  

  Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either Ramelteon H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the receptor´s re

• In contrast to RhoA Rac and Rap which are

  2021-10-20

  

  In contrast to RhoA, Rac1 and Rap1 which are stimulated by platelet activators and inhibited by NO/PKG, the GTPase ADP-ribosylation factor 6 (Arf6) is regulated in the reverse way. Platelet agonists like thrombin, collagen, or ADP, reduce Arf6-GTP levels, whereas NO and PGI2 oppose this reduction [1

• PDEs a group of metallophosphohydrolases hydrolyze the cycli

  2021-10-20

  

  PDEs, a group of metallophosphohydrolases, hydrolyze the 3′,5′-cyclic phosphate group on cyclic nucleotides to a 5′-monophosphate, thereby blocking cyclic AMP (cAMP) or cGMP signaling [8,9]. There are different types of PDE isozymes, with different substrate specificities. PDE5 (specific to cGMP) an

• br Introduction The amino acid glycine functions as a neurot

  2021-10-20

  

  Introduction The amino MK-8776 glycine functions as a neurotransmitter in the vertebrate central nervous system: as an inhibitory neurotransmitter and as a co-agonist of the NMDA-subtype of excitatory glutamatergic receptors (Eulenburg et al., 2005). Under a current hypothesis that schizophrenia

• ICH induced striatal lesion produced

  2021-10-20

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino (+)-Catechin hydrate transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain

• br Acknowledgments br Free fatty acids

  2021-10-20

  

  Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and

• br Materials and Methods br

  2021-10-20

  

  Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the

• The lack of inhibition of K efflux in

  2021-10-19

  

  The lack of inhibition of K+ efflux in normal red cells reported by Fathallah et al. [16] was attributed by the authors to a lower level (about half) of membrane PKCα activity. In our experiments, single channel recording probably overcame this difficulty because of its molecular detection level. O

• br The Farnesoid X receptor

  2021-10-19

  

  The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys

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