• Pediatric cancers are fundamentally different from

  2021-09-17

  

  Pediatric cancers are fundamentally different from adult tumors and usually display a lower mutational burden and a faster growth rate. About 30% of all childhood malignancies are solid tumors and, in a majority of cases, respond well to chemotherapy. However, in particular in neuroblastoma the succ

• By regulation of synaptic glutamate concentration glutamate

  2021-09-17

  

  By regulation of synaptic glutamate concentration, glutamate transporters play an important role in limiting glutamate signaling and controlling the activation of glutamate receptors (Rimmele and Rosenberg, 2016). Reduced glutamate transport is thought to underlie the pathogenesis of numerous neurol

• Natural product based drug discovery can be

  2021-09-17

  

  Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in ionomycin binding assays, we used molecular modeling to predict how well these compounds f

• br Results and discussion br

  2021-09-17

  

  Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust

• Both anxiety like behavior and sucrose preference intake

  2021-09-17

  

  Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo

• A great number of proteins

  2021-09-17

  

  A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous

• br Conclusion Discovery of an ideal orally active

  2021-09-17

  

  Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo

• Wolf et al then proceed to interrogate the

  2021-09-16

  

  Wolf et al. (2016) then proceed to interrogate the mechanism by which NAG activates the NLRP3 inflammasome. When examining potential triggers previously implicated in NLRP3 activation, they found that both PGN and NAG trigger appearance of mitochondrial DNA (mtDNA) in the cytosol, which led them to

• Introduction Cancer has been a

  2021-09-16

  

  Introduction Cancer has been a significant public health problem in the world with more patients being diagnosed every year. However, chemotherapy from non-specific cytotoxic agents that as an effective means of cancer treatment is limited by severe side effects and poor selectivity. Thus, the deve

• Considering that TGF plays a

  2021-09-16

  

  Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG

• br Experimental br Acknowledgements This work was financiall

  2021-09-16

  

  Experimental Acknowledgements This work was financially supported by Ministry of Knowledge and Economy (10032113) and Ministry of Education, Science and Technology (20100000297). Introduction To ensure accurate chromosome segregation, cohesion between sister chromatids must be maintained u

• The biological activity at GPR a

  2021-09-16

  

  The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu

• In the present study recipient oestradiol

  2021-09-16

  

  In the present study, recipient oestradiol serum levels on the day of donor oocyte retrieval or warming were found to be significantly higher in the antagonist group and higher than 100 pg/ml in all cases. Serum oestradiol level has been reported to have no effect on endometrial receptiveness in ooc

• The effects of these steroids namely

  2021-09-16

  

  The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the

• br Membrane transporters as a novel therapeutic

  2021-09-16

  

  Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS

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