• In an effort to increase antioxidant properties of

  2024-06-13

  

  In an effort to increase antioxidant properties of peptides from WP, Le Maux et al. (2016) altered the hydrolysis conditions (pH, enzyme type, reaction time, and temperature). Hydrolysis of WP (81% protein) test samples with papain (EC 3.4.22.2) at a constant pH of 7.0 gave significantly higher ORAC

• Hyperactivity of the hypothalamus pituitary adrenal HPA axis

  2024-06-13

  

  Hyperactivity of the hypothalamus-pituitary-adrenal (HPA) axis, which is well described in MDD (Pariante and Lightman, 2008, Marques et al., 2009), is also observed in AD and results in increased glucocorticoid (GC, cortisol in primates) levels in blood and CSF (Davis et al., 1986, Martignoni et al

• First investigation of numerous membered ether linked macroc

  2024-06-13

  

  First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin

• br Materials and method br Result

  2024-06-13

  

  Materials and method Result and discussion Conclusion Acknowledgments This work is partly supported by the University Research Committee (URC) of the Senate of The Federal University of Technology, Akure. The authors thanked IFS for the funds (F/4449 1F and F/4449-2F) used to purchase th

• br Conclusions Triptans are HT

  2024-06-13

  

  Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan

• orexin a In the vasculature it is known that A A and

  2024-06-13

  

  In the vasculature, it is known that A2A and A2B adenosine receptors are stimulatory for adenylyl-cyclase, leading to cyclic-AMP (cAMP) production and vasodilation, while the A1 and A3 adenosine receptors are linked to the inhibitory Gi, suppressing adenylyl-cyclase and favoring contraction. However

• Comparatively cell based assays appear

  2024-06-13

  

  Comparatively, cell-based assays appear to be the most sensitive method to detect patient autoantibodies directed at neurotransmitter receptors. Leite et al. demonstrated that many α-BTX RIA seronegative myasthenic patients do have autoantibodies against the AChR when a highly sensitive immunofluore

• It has been reported that

  2024-06-12

  

  It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and

• Moreover our present work suggests

  2024-06-12

  

  Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in nucleoside transporters activated with AXL receptor ligand. A ro

• Small kinase inhibitors have been developed to block AXL

  2024-06-12

  

  Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha

• br Concluding Remarks and Future Directions

  2024-06-12

  

  Concluding Remarks and Future Directions The physiological significance of autophagy in neuronal function is steadily emerging. The studies discussed herein reveal that key neuronal functions, such as neurotransmitter release, pruning of dendritic spines, and behavioural outputs of neural network

• br Results and discussion br Conclusion

  2024-06-12

  

  Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen tandospirone of

• The activity of an enzyme may

  2024-06-12

  

  The activity of an enzyme may be regulated allosterically as well as transcriptionally. We have consistently studied REMS deprivation (REMSD) associated NA mediated allosteric regulation of Na-K ATPase activity in neurons and glia in vivo and in vitro (Amar and Mallick, 2015; Amar et al., 2016; Bask

• Phagosomes acquire some hydrolases early during

  2024-06-12

  

  Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,

• We used the lead compound C to demonstrate

  2024-06-12

  

  We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.

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