• Chemotherapeutic approaches to glioblastoma which are highly

  2021-11-26

  

  Chemotherapeutic approaches to glioblastoma, which are highly invasive, are still largely unsuccessful and have only a minimal impact on patients’ survival rate . New agents that target the specific molecular aberrations in the tumors are presently being investigated for their efficacy against this

• In conclusion the data reported

  2021-11-26

  

  In conclusion, the data reported in this study have demonstrated an important role for FAAH substrates in the monoamine transporter in the modulation of TLR4-induced neuroinflammatory and associated anhedonic responses, but not acute sickness behaviour. Such potent neuroimmunomodulatory effects wer

• GSK has also been used as PET radiotracer in the

  2021-11-26

  

  GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951

• NGS substitution linkage analysis and haplotype reconstructi

  2021-11-26

  

  NGS substitution linkage analysis and haplotype reconstruction was previously only used for short genome segments and not in the context of antiviral resistance. We optimized this approach to cover a complete viral protein and major DAA target, enabling us to investigate resistance associated NS3P h

• Renal disease is characterized by aberrant fibrotic

  2021-11-26

  

  Renal disease is characterized by aberrant fibrotic remodeling of renal tissue, elevated apoptosis in kidney tissue, and eventual organ failure. In addition, patients with renal disease are more likely to suffer from systemic hypertension due to oxidative damage (reviewed in Ref. [18]). Treatment of

• It is extremely difficult to

  2021-11-26

  

  It is extremely difficult to predict a plausible conformer of hsGCαβ heterodimer with right orientation of multiple domains. Even though the template identities in case of dimeric domains were not high enough but still we modelled the entire heterodimeric structure of hsGCαβ with a reasonable and ju

• To test this concept we took advantage of our large

  2021-11-25

  

  To test this concept, we took advantage of our large supply of various 2-pyridyl containing [3.1.0] cores (inactive with alkyl or aryl sulfonamides) and prepared the -methylimidazole sulfonamide analogs and (), as work form Merck demonstrated that the 2-pyridyl moiety was superior to the original

• TXA has been shown to be

  2021-11-25

  

  TXA has been shown to be a competitive antagonist on the GABAA receptor and potentially also the glycine [7], [12], [15] receptor. Furtmuller et al. showed that TXA right-shifted the GABA CRC by one order of magnitude [7], while in our study TXA similarly right-shifted the GABA EC50 value from 0.33 

• In conclusion our work demonstrates for the

  2021-11-25

  

  In conclusion, our work demonstrates for the first time that (i) SA-β-gal activity is abundantly present in the gamete cells, such as oocytes and eggs, (ii) the enzyme resides in different cell compartments, (iii) SA-β-gal activity is localized predominantly in acidic endosomal yolk platelets, and (

• br Summary The presented results

  2021-11-25

  

  Summary The presented results of the analysis of the unfolding of G-quadruplex and i-motif, which may appear within the telomeric DNA region, led to several important conclusions. Namely, determination of the work necessary to unfold of these structures, in biased molecular dynamics involving ste

• Tail group SAR of the

  2021-11-25

  

  Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl

• So what makes a FFAR agonist different and interesting

  2021-11-25

  

  So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept

• We have presented evidence that only muscle FBPase is detect

  2021-11-25

  

  We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart phospholipase inhibitor expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our pre

• It is well known that TNF plays a

  2021-11-25

  

  It is well known that TNF-α plays a pivotal role in the pathogenesis of RA. TNF-α influences diverse pathologic processes including joint destruction as well as inflammatory responses [16]. While TNF-α significantly increases the levels of sFas and mFas expression from FLS, IL-1β and IL-17 have mini

• We have expanded these studies by doing EEG recording in

  2021-11-25

  

  We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA 46619 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist or t

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