• br Gamma secretase trafficking GS activity for

  2022-10-09

  

  Gamma-secretase trafficking GS activity for APP can be influenced by sub-cellular trafficking, as APP cleavage differs depending on its localization. APP is synthesized in the ER and transported to the trans-Golgi network (Annaert et al., 1999, Pasternak et al., 2003, Ray et al., 1999a, Rechards

• br Materials and methods br Results

  2022-10-09

  

  Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino FTI 277 HCl residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional

• The current lack of effective treatments for

  2022-10-08

  

  The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th

• Histone modification is one of the major epigenetic

  2022-10-08

  

  Histone modification is one of the major epigenetic mechanisms.8, 10 Specific histone modifications confer active or repressive transcriptional states. For instance, the trimethylation of Histone3-Lysine27 (H3K27me3) is a marker of tightly packaged heterochromatin and is associated with gene repress

• br ABT aR aR methyl hexahydropyrrolo b pyrrol yl biphenyl

  2022-10-08

  

  ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo

• A recent novel and important finding is that YAP connects

  2022-10-08

  

  A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1

• br Hydroxamic acids br Inhibitors with reporting modalities

  2022-10-04

  

  Hydroxamic acids Inhibitors with reporting modalities Dual or more HDAC inhibitors Conclusion Finally, non-human HDAC such as Schistosoma mansoni HDAC8 are targeted for parasitic diseases and recent work highlight the interest of HDACs in viral infections. Despite their discovery in the

• DMAT br Conclusion In this report we

  2022-10-04

  

  Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar

• Decreasing GSK activity has therapeutic

  2022-10-04

  

  Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic dihydrofolate reductase inhibitor antibacterial injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogeni

• br Conclusion br Acknowledgements This work was

  2022-10-04

  

  Conclusion Acknowledgements This work was supported by a Grant-in-Aid for challenging Exploratory Research (15K12715) and was a partly supported by Suzuken Memorial Foundation (2014). The authors would like to thank Enago (www.enago.jp) for the English language review. G protein-coupled rec

• Adenosine triphosphate ATP is thought to be a

  2022-10-04

  

  Adenosine triphosphate (ATP) is thought to be a crucial molecule in acute pain signaling in the DRG, as well as in the development and maintenance of chronic pain (Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). Extracellular ATP activates the ionotropic P2X receptors (Bur

• br Conflict of interest br Funding

  2022-10-04

  

  Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino Nocodazole derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-mediate

• br Regulation of Glu transporters The pivotal role

  2022-10-04

  

  Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Thalidomide calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcri

• br Experimental methods br Acknowledgments We thank all memb

  2022-10-04

  

  Experimental methods Acknowledgments We thank all members of the Hermanson lab, especially Ana Teixeira, Shirin Ilkhanizadeh and Karolina Wallenborg, for assistance and discussions, Peter Löw for anti-synaptotagmin antibody, and Lars Björklund, Ole Isacson, Christer Höög, Claes Wahlestedt and

• Analysis of the GHSR screening data

  2022-10-03

  

  Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr

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