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Identification of NQO1 and ferrochelatase as interaction partners for neuroprotective N‐{[2‐(4‐phenyl‐piperazin‐1‐yl)‐ethyl]‐phenyl}‐arylamides
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2018-04-10 , DOI: 10.1111/cbdd.13193
Sladjana-Kostic Rajacic 1 , Gerhard Schwall 2 , Jelena Penjisevic 1 , Deana Andric 3 , Vladimir Sukalovic 1 , Vukic Soskic 4
Affiliation  

Affinity chromatography was used to identify potential cellular targets that are responsible for neuroprotective activity of N‐{[2‐(4‐phenyl‐piperazin‐1‐yl)‐ethyl]‐phenyl}‐arylamides. Active and inactive representatives of N‐{[2‐(4‐phenyl‐piperazin‐1‐yl)‐ethyl]‐phenyl}‐arylamides bearing an extended linker were synthesized and immobilized on an agarose‐based matrix. This was followed by the identification of specifically bound proteins isolated out of the whole rat brain extract. Inducible flavoprotein NAD(P)H:quinone oxidoreductase (NQO1) was identified as candidates for cellular targets.

中文翻译:

鉴定NQO1和铁螯合酶作为神经保护性N-{[2-(4-苯基-哌嗪-1-基)-乙基]-苯基]-芳基酰胺的相互作用伙伴

亲和色谱用于鉴定潜在的细胞靶标,这些靶标负责N -{[2-(4-苯基-哌嗪-1-基)-乙基]-苯基}-芳基酰胺的神经保护活性。合成了带有扩展接头的N -{[2-(4-苯基哌嗪-1-基)-乙基]苯基}-苯基}-芳酰胺的活性和非活性代表,并将其固定在基于琼脂糖的基质上。接下来是鉴定从整个大鼠脑提取物中分离出的特异性结合蛋白。诱导型黄素蛋白NAD(P)H:醌氧化还原酶(NQO1)被确定为细胞靶标的候选物。
更新日期:2018-04-10
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