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Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ΔFosB homodimers and ΔFosB/JunD heterodimers.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-06-06 , DOI: 10.1016/j.bmcl.2020.127300
Yi Li 1 , Zhiqing Liu 1 , Galina Aglyamova 1 , Jianping Chen 1 , Haiying Chen 1 , Mukund Bhandari 1 , Mark A White 2 , Gabrielle Rudenko 3 , Jia Zhou 3
Affiliation  

The transcription factor ΔFosB accumulates in response to chronic insults such as drugs of abuse, L-3,4-dihydroxyphenylalanine (l-DOPA) or stress in specific regions of the brain, triggering long lasting neural and behavioral changes that underlie aspects of drug addiction, dyskinesia, and depression. Thus, small molecule chemical probes are urgently needed to investigate biological functions of ΔFosB. Herein we describe the identification of a novel phenanthridine analogue ZL0220 (27) as an active and promising ΔFosB chemical probe with micromolar inhibitory activities against ΔFosB homodimers and ΔFosB/JunD heterodimers.



中文翻译:

发现菲啶类似物作为破坏 DNA 与 ΔFosB 同源二聚体和 ΔFosB/JunD 异源二聚体结合的新型化学探针。

转录因子 ΔFosB 会因慢性损伤(例如滥用药物、L -3,4-二羟基苯丙氨酸 ( l -DOPA) 或大脑特定区域的压力)而积累,从而引发长期持久的神经和行为变化,这些变化是毒瘾的基础、运动障碍和抑郁症。因此,迫切需要小分子化学探针来研究 ΔFosB 的生物学功能。在此,我们描述了一种新型菲啶类似物 ZL0220 ( 27 )的鉴定,它是一种活性和有前途的 ΔFosB 化学探针,对 ΔFosB 同源二聚体和 ΔFosB/JunD 异源二聚体具有微摩尔抑制活性。

更新日期:2020-06-06
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