• Among prostaglandins PG PGD remained

  2022-02-09

  

  Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso

• To investigate if such an effect is observed in native

  2022-02-09

  

  To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m

• Recently unimolecular multi functional peptides that

  2022-02-08

  

  Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with EHop-016 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weight

• br Materials and methods br Results br Discussion

  2022-02-08

  

  Materials and methods Results Discussion Our data show that the ghrelin receptor, Ghsr, links energy homeostasis with a form of adult hippocampal plasticity. The presence of Ghsr on mature DG neurons suggest that acyl-ghrelin may modulate NSPCs indirectly, possibly via soluble factors such

• For the two KO models CX and CX fluorescence recovery

  2022-02-08

  

  For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular

• The regulation of gap junction connexin mediated

  2022-02-08

  

  The regulation of gap junction-connexin-mediated activities may be achieved through action on the channel gating properties (membrane voltage, pH, interaction with junctional and cytoskeletal proteins, Ca2+ and K+ concentrations, etc) or on the trafficking, turnover and localization of connexins. Sh

• Also a large number of small

  2022-02-08

  

  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 [

• Drosophila is a well established model to

  2022-02-08

  

  Drosophila is a well-established model to investigate the molecular and cellular defects underlying human neurodevelopmental disorders (Oortveld et al., 2013, van der Voet et al., 2014). Here, we establish Drosophila as a model for understanding the mechanisms linking mutations in KDM5 family protei

• Although epigenetic mechanisms are implicated in the

  2022-02-08

  

  Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de

• To efficiently develop bioactive ligands even

  2022-02-08

  

  To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s

• br Although there are growing

  2022-02-08

  

  Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a

• IAA-94 The first suggestion that the

  2022-02-08

  

  The first suggestion that the Hh pathway might be involved in the pathogenesis of chronic liver disease was reported at the beginning of this millennium by Shackel et al. who noted that Patch and Gli were upregulated in their microarray analysis of liver tissues from patients with primary biliary ch

• FSH and LH are glycoprotein

  2022-02-07

  

  FSH and LH, are glycoprotein dimers that are comprised of two subunits, a common α-subunit (αGSU) and a distinct β-subunit (FSHβ or LHβ, respectively), which determines the biological specificity of the gonadotropins (Ciccone and Kaiser, 2009, Gharib et al., 1990). The terazosin hcl of the gonadotro

• Post translational ubiquitination has been shown to

  2022-02-07

  

  Post-translational ubiquitination has been shown to regulate a wide range of cellular responses, such as the synaptic trafficking and turnover of neurotransmitter receptors (Rape, 2018). Ubiquitination is also engaged in the modification of protein-protein interaction and intracellular signaling tra

• The third generation cephalosporin antibiotics

  2022-02-07

  

  The third-generation cephalosporin Bay 65-1942 HCl salt receptor can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when

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