Design, synthesis, and neuroprotective effects of a dimeric dipeptide mimetic of the third loop of the nerve growth factor
作者: T. A. GudashevaA. V. TarasiukN. M. SazonovaS. V. PomogaiboA. N. ShumskiyI. O. LogvinovS. V. NikolaevP. Yu. PovarninaM. A. KonstantinopolskyT. A. AntipovaS. B. Seredenin
作者单位: 1Zakusov Research Institute of Pharmacology
刊名: Russian Journal of Bioorganic Chemistry, 2017, Vol.43 (3), pp.235-247
来源数据库: Springer Nature Journal
DOI: 10.1134/S1068162017030050
关键词: NGFMimeticThe GTS-115 dipeptideNeuroprotective activityMAPK/ERKPI3K/AKT
原始语种摘要: Previously, we prepared dimeric dipeptide mimetics of the first and the fourth loops of the nerve growth factor (NGF): hexamethylenediamides of bis( N -aminocaproyl-glycyl-L-lysine) (GK-6) and bis( N -monosuccinyl-L-glutamyl-L-lysine) (GK-2). Both mimetics activated TrkA-receptors, but induced different postreceptor signal pathways. GK-2 selectively activated PI3K/AKT, whereas GK-6 activated both PI3K/AKT and MAPK/ERK. Both mimetics exhibited a neuroprotective activity. In this study, we continued the investigation of a contribution of separate loop-like structures in the NGF functions and created and studied dimeric dipeptide mimetics based on a beta-turn of the NGF third loop: hexamethylenediamides of bis( N -gamma-hydroxybutyryl-L-lysyl-L-histidine) (GTS-115) and bis( N...
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影响因子:0.523 (2012)

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关键词翻译
关键词翻译
  • mimetic 模仿的
  • dipeptide 二肽
  • dimeric 二聚的
  • nerve 叶脉
  • synthesis 合成
  • inhibitory 禁止的
  • NGF Navigation Flare
  • lysyl 赖氨酰基
  • induced 感应的
  • third 第三的